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779 Cards in this Set

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Time it takes for amount of drug to fall to half of its value, constant in first order kinetics (majority of drugs)
*Half-life (T1/2)
basic pharmacokinetics
Relates the amount of drug in the body to the plasma concentration
Volume of distribution (VD)
basic pharmacokinetics
Plasma concentration of a drug at a given time
Cp
basic pharmacokinetics
The ratio of the rate of elimination of a drug to its plasma concentration
Clearance (CL)
basic pharmacokinetics
The elimination of drug that occurs before it reaches the systemic circulation
First pass effect
basic pharmacokinetics
The fraction of administered dose of a drug that reaches systemic circulation
Bioavailability (F)
basic pharmacokinetics
When the rate of drug input equals the rate of drug elimination
Steady state
basic pharmacokinetics
This step of metabolism makes drug more hydrophilic and hence augments elimination
*Phase I
metabolism
Different steps of Phase I
Oxidation, reduction, hydrolysis
metabolism
Inducers of Cytochrome P450 (CYP450)
*Barbiturates, phenytoin, carbamazepine, and rifampin
metabolism
Inhibitors of CYP450
*Cimetidine, ketoconazole, erythromycin, isoniazid and grapefruit
metabolism
Products of Phase II conjugation
Glucuronate, acetic acid, and glutathione sulfate
metabolism
Constant percentage of substrate metabolized per unit time
First order kinetics
metabolism
Drug elimination with a constant amount metabolized regardless of drug concentration
Zero order kinetics
metabolism
Target plasma concentration times (volume of distribution divided by bioavailability)
Loading dose (Cp*(Vd/F))
metabolism
Concentration in the plasma times (clearance divided by bioavailability)
Maintenance dose (Cp*(CL/F))
metabolism
Strength of interaction between drug and its receptor
Affinity
pharmacodynamics
Selectivity of a drug for its receptor
Specificity
pharmacodynamics
Amount of drug necessary to elicit a biologic effect
Potency
pharmacodynamics
Ability of drug to produce a biologic effect
*Efficacy
pharmacodynamics
Ability of a drug to produce 100% of the maximum response regardless of the potency
Full agonist
pharmacodynamics
Ability to produce less than 100% of the response
Partial agonist
pharmacodynamics
Ability to bind reversibly to the same site as the drug and without activating the effector system
Competitive antagonist
pharmacodynamics
Ability to bind to either the same or different site as the drug
Noncompetitive antagonist
pharmacodynamics
Mechanism of action (MOA) utilizes intracellular receptors
*Thyroid and steroid hormones
pharmacodynamics
MOA utilizes transmembrane receptors
*Insulin
pharmacodynamics
MOA utilizes ligand gated ion channels
Benzodiazepines and calcium channel blockers
pharmacodynamics
Median effective dose required for an effect in 50% of the population
ED50
pharmacodynamics
Median toxic dose required for a toxic effect in 50% of the population
TD50
pharmacodynamics
Dose which is lethal to 50% of the population
LD50
pharmacodynamics
Window between therapeutic effect and toxic effect
Therapeutic index
pharmacodynamics
Drug with a high margin of safety
High therapeutic index
pharmacodynamics
Drug with a narrow margin of safety
Low therapeutic index
pharmacodynamics
Antidote used for lead poisoning
Dimercaprol, EDTA
antidotes and agents used in drug overdose
Antidote used for cyanide poisoning
Nitrites
antidotes and agents used in drug overdose
Antidote used for anticholinergic poisoning
Physostigmine
antidotes and agents used in drug overdose
Antidote used for organophosphate/anticholinesterase poisoning
**Atropine, pralidoxime (2-PAM)
antidotes and agents used in drug overdose
Antidote used for iron salt toxicity
Deferoxamine
antidotes and agents used in drug overdose
Antidote used for acetaminophen (APAP) toxicity
*N-acetylcysteine (Mucomyst)
antidotes and agents used in drug overdose
Antidote for arsenic, mercury, lead, and gold poisoning
Dimercaprol
antidotes and agents used in drug overdose
Antidote used in poisonings: copper (Wilson's disease), lead, mercury, and arsenic
Penicillamine
antidotes and agents used in drug overdose
Antidote used for heparin toxicity
**Protamine
antidotes and agents used in drug overdose
Antidote used for warfarin toxicity
*Vitamin K and Fresh frozen plasma (FFP)
antidotes and agents used in drug overdose
Antidote for tissue plasminogen activator (t-PA), streptokinase
**Aminocaproic acid
antidotes and agents used in drug overdose
Antidote used for methanol and ethylene glycol
Ethanol
antidotes and agents used in drug overdose
Antidote used for opioid toxicity
*Naloxone (IV), naltrexone (PO)
antidotes and agents used in drug overdose
Antidote used for benzodiazepine toxicity
*Flumazenil
antidotes and agents used in drug overdose
Antidote used for tricyclic antidepressants (TCA)
Sodium bicarbonate
antidotes and agents used in drug overdose
Antidote used for carbon monoxide poisoning
100% O2 and hyperbaric O2
antidotes and agents used in drug overdose
Antidote used for digitalis toxicity
Digibind (also need to d/c digoxin, normalize K+, and lidocaine if pt. Is arrhythmic)
antidotes and agents used in drug overdose
Antidote used for beta agonist toxicity (eg. Metaproterenol)
Esmolol
antidotes and agents used in drug overdose
Antidote for methotrexate toxicity
Leucovorin
antidotes and agents used in drug overdose
Antidote for beta-blockers and hypoglycemia
Glucagon
antidotes and agents used in drug overdose
Antidote useful for some drug induced Torsade de pointes
Magnesium sulfate
antidotes and agents used in drug overdose
Antidote for hyperkalemia
sodium polystyrene sulfonate (Kayexalate)
antidotes and agents used in drug overdose
Antidote for salicylate intoxication
Alkalinize urine, dialysis
antidotes and agents used in drug overdose
Constant proportion of cell population killed rather than a constant number
Log-kill hypothesis
cancer chemotherapy
Treatment with cancer chemotherapy at high doses every 3-4 weeks, too toxic to be used continuously
Pulse therapy
cancer chemotherapy
Toxic effect of anticancer drug can be lessened by rescue agents
Rescue therapy
cancer chemotherapy
Drug used concurrently with toxic anticancer agents to reduce renal precipitation of urates
Allopurinol
cancer chemotherapy
Pyrimidine analog that causes "Thiamine-less death" given with leucovorin rescue
5-flouracil (5-FU)
cancer chemotherapy
Drug used in cancer therapy causes Cushing-like symptoms
Prednisone
cancer chemotherapy
Side effect of Mitomycin
SEVERE myelosuppression
cancer chemotherapy
MOA of cisplatin
Alkylating agent
cancer chemotherapy
Common toxicities of cisplatin
Nephro and ototoxicity
cancer chemotherapy
Analog of hypoxanthine, needs HGPRTase for activation
6-mercaptopurine (6-MP)
cancer chemotherapy
Interaction with this drug requires dose reduction of 6-MP
**Allopurinol
cancer chemotherapy
May protect against doxorubicin toxic by scavenging free radicals
*Dexrazoxane
cancer chemotherapy
Blows DNA (breaks DNA strands), limiting SE is pulmonary fibrosis
*Bleomycin
cancer chemotherapy
Bleomycin+vinblastine+etoposide+cisplatin produce almost a 100% response when all agents are used for this neoplasm
Testicular cancer
cancer chemotherapy
MOPP regimen used in Hodgkin's disease (HD)
Mechlorethamine+ oncovorin (vincristine)+ procarbazine, and prednisone
cancer chemotherapy
ABVD regimen used for HD, but appears less likely to cause sterility and secondary malignancies than MOPP
Adriamycin (doxorubicin) +bleomycin, vinblastine +dacarbazine
cancer chemotherapy
Regimen used for non-Hodgkin's lymphoma
COP (cyclophosphamide, oncovin(vincristine), and prednisone)
cancer chemotherapy
Regimen used for breast cancer
CMF (cyclophosphamide, methotrexate, and fluorouracil) and tamoxifen if ER+
cancer chemotherapy
Alkylating agent, vesicant that causes tissue damage with extravasation
Mechlorethamine
cancer chemotherapy
Anticancer drug also used in RA, produces acrolein in urine that leads to hemorrhagic cystitis
Cyclophosphamide
cancer chemotherapy
Prevention of cyclophosphamide induced hemorrhagic cystitis
Hydration and mercaptoethanesulfonate (MESNA)
cancer chemotherapy
Microtubule inhibitor that causes peripheral neuropathy, foot drop (eg. ataxia), and "pins and needles" sensation
Vincristine
cancer chemotherapy
Interact with microtubules (but unlike vinca which prevent disassembly of tubules), it stabilizes tubulin and cells remain frozen in metaphase
**Paclitaxel (taxol)
cancer chemotherapy
Toxicities include nephrotoxicity and ototoxicity, leading to a severe interaction with aminoglycosides
Cisplatin
cancer chemotherapy
Agent similar to cisplatin, less nephrotoxic, but greater myelosuppression
Carboplatin
cancer chemotherapy
Converts asparagine to aspartate and ammonia, denies cancer cells of essential AA (asparagine)
L-asparaginase
cancer chemotherapy
Used for hairy cell leukemia; it stimulates NK cells
Interferon alpha
cancer chemotherapy
Anti-androgen used for prostate cancer
Flutamide (Eulexin)
cancer chemotherapy
Anti-estrogen used for estrogen receptor + breast cancer
**Tamoxifen
cancer chemotherapy
Newer estrogen receptor antagonist used in advanced breast cancer
Toremifene (Fareston)
cancer chemotherapy
Some cell cycle specific anti-cancer drugs
Bleomycin, vinca alkaloids, antimetabolites (eg., 5-FU, 6-MP, methotrexate, etoposide)
cancer chemotherapy
Some cell cycle non-specific drugs
Alkylating agents (eg., mechlorethamine, cyclophosphamide), antibiotics (doxorubicin, daunorubicin), cisplatin, nitrosourea
cancer chemotherapy
Anti-emetics used in association with anti-cancer drugs that are 5-HT3 (serotonin receptor subtype ) antagonist
*Odansetron, granisetron
cancer chemotherapy
Nitrosoureas with high lipophilicity, used for brain tumors
Carmustine (BCNU) and lomustine (CCNU)
cancer chemotherapy
Produces disulfiram-like reaction with ethanol
Procarbazine
cancer chemotherapy
Somatostatin (SRIF) analog used for acromegaly, carcinoid, glucagonoma and other GH producing pituitary tumors
Octreotide
endocrine drugs: hypothalamic and pituitary hormones
Somatotropin (GH) analog used in GH deficiency (dwarfism)
Somatrem
endocrine drugs: hypothalamic and pituitary hormones
GHRH analog used as diagnostic agent
Sermorelin
endocrine drugs: hypothalamic and pituitary hormones
GnRH agonist used for infertility or different types of CA depending on pulsatile or steady usage respectively
Leuprolide
endocrine drugs: hypothalamic and pituitary hormones
GnRH antagonist with more immediate effects, used for infertility
Ganirelix
endocrine drugs: hypothalamic and pituitary hormones
Dopamine (DA) agonist (for Parkinson's disease), used also for hyperprolactinemia
*Bromocriptine
endocrine drugs: hypothalamic and pituitary hormones
Hormone inhibiting prolactin release
*Dopamine
endocrine drugs: hypothalamic and pituitary hormones
ACTH analog used for diagnosis of patients with corticosteroid abnormality
**Cosyntropin
endocrine drugs: hypothalamic and pituitary hormones
Synthetic analog of ADH hormone used for diabetes insipidus and nocturnal enuresis
*Desmopressin (DDAVP)
endocrine drugs: hypothalamic and pituitary hormones
Most widely used thyroid drugs such as Synthroid and Levoxyl contain
**L-thyroxine (T4)
thyroid / anti-thyroid
T3 compound less widely used
Cytomel
thyroid / anti-thyroid
Anti-thyroid drugs
Thioamides, iodides, radioactive iodine, and ipodate
thyroid / anti-thyroid
Thioamide agents used in hyperthyroidism
Methimazole and propylthiouracil (PTU)
thyroid / anti-thyroid
Thioamide less likely to cross placenta, inhibits peripheral conversion of T4 to T3 in high doses, and should be used with extreme caution in pregnancy
*PTU
thyroid / anti-thyroid
PTU (propylthiouracil) MOA
*Inhibits thyroid hormone synthesis by blocking iodination of the tyrosine residues of thyroglobulin
thyroid / anti-thyroid
Can be effective for short term therapy of thyroid storm, but after several weeks of therapy causes an exacerbation of hyperthyroidism
Iodide salts
thyroid / anti-thyroid
Permanently cures thyrotoxicosis, patients will need thyroid replacement therapy thereafter. Contraindicated in pregnancy
Radioactive iodine
thyroid / anti-thyroid
Radio contrast media that inhibits the conversion of T4 to T3
Ipodate
thyroid / anti-thyroid
Block cardiac adverse effects of thyrotoxicosis such as tachycardia, inhibits the conversion of T4 to T3
Beta-blockers such as propranolol
thyroid / anti-thyroid
3 zones of adrenal cortex and their products
Glomerulosa (mineralocorticoids), fasciculata (glucocorticoid=GC), and reticularis (adrenal androgens)
Adrenocorticosteroid and adrenocortical antagoinists
Pneumonic for 3 zones of adrenal cortex
GFR
Adrenocorticosteroid and adrenocortical antagoinists
Used for Addison's disease, Congenital Adrenal Hyperplasia (CAH), inflammation, allergies, and asthma (as a local inhalation)
Glucocorticoids
Adrenocorticosteroid and adrenocortical antagoinists
Short acting GC's
Cortisone and hydrocortisone (equivalent to cortisol)
Adrenocorticosteroid and adrenocortical antagoinists
Intermediate acting GC's
Prednisone, methylprednisolone, prednisolone, and triamcinolone
Adrenocorticosteroid and adrenocortical antagoinists
Long acting GC's
Betamethasone, dexamethasone, and paramethasone
Adrenocorticosteroid and adrenocortical antagoinists
Mineralocorticoids
Fludrocortisone and deoxycorticosterone
Adrenocorticosteroid and adrenocortical antagoinists
Some side effects of corticosteroids
*Osteopenia, impaired wound healing, inc. risk of infection, inc. appetite, HTN, edema, PUD, euphoria, psychosis
Adrenocorticosteroid and adrenocortical antagoinists
Period of time of therapy after which GC therapy will need to be tapered
5-7 days
Adrenocorticosteroid and adrenocortical antagoinists
Used for Cushing's syndrome (increased corticosteroid) and sometimes for adrenal function test
Metyrapone
inhib of corticosteroid biosynth
Inhibits conversion of cholesterol to pregnenolone therefore inhibiting corticosteroid synthesis
Aminoglutethimide
inhib of corticosteroid biosynth
Antifungal agent used for inhibition of all gonadal and adrenal steroids
Ketoconazole
inhib of corticosteroid biosynth
Antiprogestin used as potent antagonist of GC receptor
Mifepristone
inhib of corticosteroid biosynth
Diuretic used to antagonize aldosterone receptors
*Spironolactone
inhib of corticosteroid biosynth
Common SE of spironolactone
**Gynecomastia and hyperkalemia
inhib of corticosteroid biosynth
Slightly increased risk of breast cancer, endometrial cancer, heart disease (questionable), has beneficial effects on bone loss
Estrogen
gonadal hormones and inhib
Antiestrogen drugs used for fertility and breast cancer respectively
Clomiphene and tamoxifen
gonadal hormones and inhib
Common SE of tamoxifen and raloxifene
Hot flashes
gonadal hormones and inhib
Selective estrogen receptor modulator (SERM) used for prevention of osteoporosis and currently being tested for treatment of breast cancer (Stars study)
**Raloxifene
gonadal hormones and inhib
Non-steroidal estrogen agonist causes clear cell adenocarcinoma of the vagina in daughters of women who used it during pregnancy
*Diethylstilbestrol (DES)
gonadal hormones and inhib
Estrogen mostly used in oral contraceptives (OC)
Ethinyl estradiol and mestranol
gonadal hormones and inhib
Anti-progesterone used as abortifacient
Mifepristone (RU-486)
gonadal hormones and inhib
Constant low dose of estrogen and increasing dose of progestin for 21 days (last 5 days are sugar pills or iron prep)
Combination oral contraceptives (OC)
gonadal hormones and inhib
Oral contraceptive available in a transdermal patch
Ortho-Evra
gonadal hormones and inhib
Converted to more active form DHT by 5 alpha-reductase
*Testosterone
gonadal hormones and inhib
5 alpha-reductase inhibitor used for benign prostatic hyperplasia (BPH) and male pattern baldness
Finasteride (Proscar and Propecia respectively)
gonadal hormones and inhib
Anabolic steroid that has potential for abuse
Nandrolone and stanozolol
gonadal hormones and inhib
Anti-androgen used for hirsutism in females
Cyproterone acetate
gonadal hormones and inhib
Drug is used with testosterone for male fertility
**Leuprolide
gonadal hormones and inhib
Alpha cells in the pancreas
Produce glucagon
pancreatic hormones, antidiabetics, and hyperglycemics
Beta cells in the pancreas
Produce insulin
pancreatic hormones, antidiabetics, and hyperglycemics
Beta cells are found
Islets of Langerhans
pancreatic hormones, antidiabetics, and hyperglycemics
Delta cells in the pancreas
Produce Somatostatin
pancreatic hormones, antidiabetics, and hyperglycemics
Product of proinsulin cleavage used to assess insulin abuse
*C-peptide
pancreatic hormones, antidiabetics, and hyperglycemics
Exogenous insulin
*Little C-peptide
pancreatic hormones, antidiabetics, and hyperglycemics
Endogenous insulin
Normal C-peptide
pancreatic hormones, antidiabetics, and hyperglycemics
Very rapid acting insulin, having fastest onset and shortest duration of action
Lispro (Humalog)
pancreatic hormones, antidiabetics, and hyperglycemics
Rapid acting, crystalline zinc insulin used to reverse acute hyperglycemia
Regular (Humulin R)
pancreatic hormones, antidiabetics, and hyperglycemics
Long acting insulin
*Ultralente (humulin U)
pancreatic hormones, antidiabetics, and hyperglycemics
Ultra long acting insulin, has over a day duration of action
Glargine (Lantus)
pancreatic hormones, antidiabetics, and hyperglycemics
Major SE of insulin
Hypoglycemia
pancreatic hormones, antidiabetics, and hyperglycemics
Important in synthesis of glucose to glycogen in the liver
GLUT 2
pancreatic hormones, antidiabetics, and hyperglycemics
Important in muscle and adipose tissue for glucose transport across muscles and TG storage by lipoprotein lipase activation
GLUT 4
pancreatic hormones, antidiabetics, and hyperglycemics
Examples of alpha-glucosidase inhibitors (AGI)
Acarbose, miglitol
pancreatic hormones, antidiabetics, and hyperglycemics
MOA of AGI's
Act on intestine, delay absorption of glucose
pancreatic hormones, antidiabetics, and hyperglycemics
SE of AGI's
Flatulence (do not use beano to tx), diarrhea, abdominal cramps
pancreatic hormones, antidiabetics, and hyperglycemics
Alpha-glucosidase inhibitor associated with elevation of LFT's
Acarbose
pancreatic hormones, antidiabetics, and hyperglycemics
Amino acid derivative
*Nateglinide
pancreatic hormones, antidiabetics, and hyperglycemics
MOA of nateglinide
Insulin secretagogue
pancreatic hormones, antidiabetics, and hyperglycemics
Biguanide
Metformin
pancreatic hormones, antidiabetics, and hyperglycemics
Drugs available in combination with metformin
Glyburide, glipizide, and rosiglitazone
pancreatic hormones, antidiabetics, and hyperglycemics
MOA of metformin
Decreases hepatic glucose production and intestinal glucose absorption; increase insulin sensitivity
pancreatic hormones, antidiabetics, and hyperglycemics
Most important potential SE of metformin
Lactic acidosis
pancreatic hormones, antidiabetics, and hyperglycemics
Meglitinide
Repaglinide
pancreatic hormones, antidiabetics, and hyperglycemics
MOA of repaglinide
Insulin release from pancreas; faster and shorter acting than sulfonylurea
pancreatic hormones, antidiabetics, and hyperglycemics
First generation sulfonylurea
Chlorpropamide, tolbutamide, tolazamide, etc.
pancreatic hormones, antidiabetics, and hyperglycemics
Second generation sulfonylurea
Glyburide, glipizide, glimepiride, etc.
pancreatic hormones, antidiabetics, and hyperglycemics
MOA of both generations
Insulin release from pancreas by modifying K+ channels
pancreatic hormones, antidiabetics, and hyperglycemics
Common SE of sulfonylureas, repaglinide, and nateglinide
Hypoglycemia
pancreatic hormones, antidiabetics, and hyperglycemics
Sulfonylurea NOT recommended for elderly because of very long half life
Chlorpropamide
pancreatic hormones, antidiabetics, and hyperglycemics
Thiazolidinediones
Pioglitazone, Rosiglitazone, Troglitazone (withdrawn/d from market)
pancreatic hormones, antidiabetics, and hyperglycemics
Reason troglitazone was withdrawn from market
Hepatic toxicity
pancreatic hormones, antidiabetics, and hyperglycemics
MOA of thiazolindinediones
Stimulate PPAR-gamma receptor to regulate CHO and lipid metabolism
pancreatic hormones, antidiabetics, and hyperglycemics
SE of Thiazolindinediones
Edema, mild anemia; interaction with drugs that undergo CytP450 3A4 metabolism
pancreatic hormones, antidiabetics, and hyperglycemics
Hyperglycemic agent that increases cAMP and results in glycogenolysis, gluconeogenesis, reverses hypoglycemia, also used to reverse severe beta-blocker overdose and smooth muscle relaxation
Glucagon
pancreatic hormones, antidiabetics, and hyperglycemics
Available bisphosphonates
Alendronate, etidronate, risedronate, pamidronate, tiludronate, and zoledronic acid
drugs used in bone homeostasis
MOA of Bisphosphonates
Inhibits osteoclast bone resorption
drugs used in bone homeostasis
Only bisphosphonates available IV
Etidronate
drugs used in bone homeostasis
Uses of bisphosphonates
Osteoporosis, Paget's disease, and osteolytic bone lesions, and hypercalcemia from malignancy
drugs used in bone homeostasis
Major SE of bisphosphonates
Chemical esophagitis
drugs used in bone homeostasis
Bisphosphonates that cannot be used on continuous basis because it caused osteomalacia
Etidronate
drugs used in bone homeostasis
Used for prevention of postmenopausal osteoporosis in women
Estrogen (HRT-Hormone replacement therapy)
drugs used in bone homeostasis
Increase bone density, also being tested for breast CA tx.
**Raloxifene (SERM-selective estrogen receptor modulator)
drugs used in bone homeostasis
Used intranasally and decreases bone resorption
*Calcitonin (salmon prep)
drugs used in bone homeostasis
Used especially in postmenopausal women, dosage should be 1500 mg
Calcium
drugs used in bone homeostasis
Vitamin given with calcium to ensure proper absorption
Vitamin D
drugs used in bone homeostasis
Disease caused by excess ergot alkaloids
St. Anthony's Fire
drugs w/ important actions on smooth muscle
Endogenous substances commonly interpreted as histamine, serotonin, prostaglandins, and vasoactive peptides
Autocoids
drugs w/ important actions on smooth muscle
Syndrome of hypersecretion of gastric acid and pepsin usually caused by gastrinoma; it is associated with severe peptic ulceration and diarrhea
Zollinger-Ellison Syndrome
drugs w/ important actions on smooth muscle
Drug that causes contraction of the uterus
*Oxytocin
drugs w/ important actions on smooth muscle
Distribution of histamine receptors H1, H2, and H3
*Smooth muscle; stomach, heart, and mast cells; nerve endings, CNS respectively
drugs w/ important actions on smooth muscle
Prototype antagonist of H1 and H2 receptors
*Diphenhydramine and impromidine respectively
drugs w/ important actions on smooth muscle
1st generation antihistamine that is highly sedating
**Diphendydramine
drugs w/ important actions on smooth muscle
1st generation antihistamine that is least sedating
Chlorpheniramine or cyclizine
drugs w/ important actions on smooth muscle
2nd generation antihistamines
*Fexofenadine, loratadine, and cetirizine
drugs w/ important actions on smooth muscle
Generation of antihistamine that has the most CNS effects
First generation due to being more lipid-soluble
drugs w/ important actions on smooth muscle
Major indication for H1 receptor antagonist
Use in IgE mediated allergic reaction
drugs w/ important actions on smooth muscle
Antihistamine that can be used for anxiety and insomnia and is not addictive
hydroxyzine (Atarax)
drugs w/ important actions on smooth muscle
H1 antagonist used in motion sickness
Dimenhydrinate, meclizine, and other 1st generation
drugs w/ important actions on smooth muscle
Most common side effect of 1st generation antihistamines
Sedation
drugs w/ important actions on smooth muscle
Lethal arrhythmias resulting from concurrent therapy with azole fungals (metabolized by CYP 3A4) and these antihistamines which inhibit the 3A4 iso-enzyme.
Terfenadine and astemizole (have been removed from the market)
drugs w/ important actions on smooth muscle
H2 blocker that causes the most interactions with other drugs
*Cimetidine
drugs w/ important actions on smooth muscle
Clinical use for H2 blockers
Acid reflux disease, duodenal ulcer and peptic ulcer disease
drugs w/ important actions on smooth muscle
Receptors for serotonin (5HT-1) are located
Mostly in the brain, and they mediate synaptic inhibition via increased K+ conductance
drugs w/ important actions on smooth muscle
5HT-1d agonist used for migraine headaches "
**Sumatriptan, naratriptan, and rizatriptan
drugs w/ important actions on smooth muscle
Triptan available in parenteral and nasal formulation
Sumatriptan
drugs w/ important actions on smooth muscle
H1 blocker that is also a serotonin antagonist
Cyproheptadine
drugs w/ important actions on smooth muscle
5HT2 antagonist mediate synaptic excitation in the CNS and smooth muscle contraction
Ketanserin, cyproheptadine, and ergot alkaloids (partial agonist of alpha and serotonin receptors)
drugs w/ important actions on smooth muscle
Agents for reduction of postpartum bleeding
**Ergonovine and ergotamine
drugs w/ important actions on smooth muscle
Agents used in treatment of carcinoid tumor
**Ketanserin cyproheptadine, and phenoxybenzamine
drugs w/ important actions on smooth muscle
5HT-3 antagonist used in chemotherapeutic induced emesis
***Ondansetron, granisetron, dolasetron and alosetron
drugs w/ important actions on smooth muscle
5ht-3 antagonist that has been associated with QRS and QTc prolongation and should not be used in patients with heart disease
Dolasetron
drugs w/ important actions on smooth muscle
DOC of chemo induced nausea and vomiting
**Odansetron
drugs w/ important actions on smooth muscle
Drug used in ergot alkaloids overdose, ischemia and gangrene
Nitroprusside
drugs w/ important actions on smooth muscle
Reason ergot alkaloids are contraindicated in pregnancy
Uterine contractions
drugs w/ important actions on smooth muscle
SE of ergot alkaloids
Hallucinations resembling psychosis
drugs w/ important actions on smooth muscle
Ergot alkaloid used as an illicit drug
*LSD
drugs w/ important actions on smooth muscle
Dopamine agonist used in hyperprolactinemia
*Bromocriptine
drugs w/ important actions on smooth muscle
Peptide causing increased capillary permeability and edema
Bradykinin and histamine
drugs w/ important actions on smooth muscle
Mediator of tissue pain, edema, inactivated by ACE, and may be a contributing factor to the development of angioedema
*Bradykinin
drugs w/ important actions on smooth muscle
Drug causing depletion of substance P (vasodilator)
*Capsaicin
drugs w/ important actions on smooth muscle
Prostaglandins that cause abortions
*Prostaglandin E1 (misoprostol) PGE2, and PGF2alpha
drugs w/ important actions on smooth muscle
Difference between COX 1 and COX 2
COX 1 is found throughout the body and COX 2 is only in inflammatory tissue
drugs w/ important actions on smooth muscle
Drug that selectively inhibits COX 2
Celecoxib, valdecoxib, and rofecoxib
drugs w/ important actions on smooth muscle
Inhibitor of lipoxygenase
*Zileuton
drugs w/ important actions on smooth muscle
Major SE of zileuton
Liver toxicity
drugs w/ important actions on smooth muscle
Inhibitor of leukotrienes (LTD4) receptors and used in asthma
Zafirlukast and montelukast
drugs w/ important actions on smooth muscle
Used in pediatrics to maintain patency of ductus arteriosis
*PGE1
drugs w/ important actions on smooth muscle
Approved for use in severe pulmonary HTN
PGI2 (epoprostenol)
drugs w/ important actions on smooth muscle
Prostaglandin used in the treatment impotence
*Alprostadil
drugs w/ important actions on smooth muscle
Irreversible, nonselective COX inhibitor
Aspirin
drugs w/ important actions on smooth muscle
Class of drugs that reversibly inhibit COX
NSAIDS
drugs w/ important actions on smooth muscle
Primary endogenous substrate for Nitric Oxidase Synthase
Arginine
drugs w/ important actions on smooth muscle
MOA and effect of nitric oxide
*Stimulates cGMP which leads to vascular smooth muscle relaxation
drugs w/ important actions on smooth muscle
Long acting beta 2 agonist used in asthma
Salmeterol
drugs w/ important actions on smooth muscle
Muscarinic antagonist used in asthma
*Ipratropium
drugs w/ important actions on smooth muscle
MOA action of cromolyn
*Mast cell stabilizer
drugs w/ important actions on smooth muscle
Enzyme which theophylline inhibits
Phosphodiesterase
drugs w/ important actions on smooth muscle
Methylxanthine derivative used as a remedy for intermittent claudication
Pentoxifylline
drugs w/ important actions on smooth muscle
Antidote for severe CV toxicity of theophylline
Beta blockers
drugs w/ important actions on smooth muscle
MOA of corticosteroids"
inhibit phospholipase A2
drugs w/ important actions on smooth muscle
SE of long term (>5 days) corticosteroid therapy and remedy
*Adrenal suppression and weaning slowly, respectively
drugs w/ important actions on smooth muscle
MOA of quinolones
**Inhibit DNA gyrase
antimicrobials
MOA of penicillin
Block cell wall synthesis by inhibiting peptidoglycan cross-linkage
antimicrobials
Drug used for MRSA
*Vancomycin
antimicrobials
Vancomycin MOA
**Blocks peptidoglycan synthesis
antimicrobials
Type of resistance found with vancomycin
Point mutation
antimicrobials
Meningitis prophylaxis in exposed patients
*Rifampin
antimicrobials
Technique used to diagnose perianal itching, and the drug used to treat it
*Scotch tape technique and mebendazole
antimicrobials
Two toxicities of aminoglycosides
nephro and ototoxicity
antimicrobials
DOC for Legionnaires' disease
Erythromycin
antimicrobials
MOA of sulfonamides
*Inhibit dihydropteroate synthase
antimicrobials
Penicillins active against penicillinase secreting bacteria
Methicillin, nafcillin, and dicloxacillin
antimicrobials
Cheap wide spectrum antibiotic DOC of otitis media
**Amoxicillin
antimicrobials
Class of antibiotics that have 10% cross sensitivity with penicillins
Cephalosporins
antimicrobials
PCN active against pseudomonas
Carbenicillin, piperacillin and ticarcillin
antimicrobials
Antibiotic causing red-man syndrome, and prevention
Vancomycin, infusion at a slow rate and antihistamines
antimicrobials
Drug causes teeth discoloration
Tetracycline
antimicrobials
MOA of tetracycline
Decreases protein synthesis by inhibiting 30S ribosome
antimicrobials
Drug that causes gray baby syndrome and aplastic anemia
Chloramphenicol
antimicrobials
Drug notorious for causing pseudomembranous colitis
Clindamycin
antimicrobials
DOC for tx of pseudomembranous colitis
**Metronidazole
antimicrobials
Treatment of resistant pseudomembranous colitis
ORAL vancomycin
antimicrobials
Anemia caused by trimethoprim
*Megaloblastic anemia
antimicrobials
Reason fluoroquinolones are contraindicated in children and pregnancy
Cartilage damage
antimicrobials
DOC for giardia, bacterial vaginosis, pseudomembranous colitis, and trichomonas
*Metronidazole
antimicrobials
Treatment for TB patients (think RIPE)
*Rifampin, Isoniazid, Pyrazinamide, and Ethambutol
antimicrobials
Metronidazole SE if given with alcohol
Disulfiram-like reaction
antimicrobials
Common side effect of Rifampin
*Red urine discoloration
antimicrobials
MOA of nystatin
Bind ergosterol in fungal cell membrane
antimicrobials
Neurotoxicity with isoniazid (INH) prevented by
Administration of Vit. B6 (pyridoxine)
antimicrobials
Toxicity of amphotericin
Nephrotoxicity
antimicrobials
SE seen only in men with administration of ketoconazole
Gynecomastia
antimicrobials
Topical DOC in impetigo
Topical mupirocin (Bactroban)
antimicrobials
DOC for influenza A
*Amantadine
antimicrobials
DOC for RSV
*Ribavirin
antimicrobials
DOC for CMV retinitis
Ganciclovir
antimicrobials
SE for ganciclovir
Neutro, leuko and thrombocytopenia
antimicrobials
Anti-viral agents associated with Stephen Johnson syndrome
Nevirapine, amprenavir
antimicrobials
HIV antiviral class known to have severe drug interactions by causing inhibition of metabolism
*Protease inhibitors
antimicrobials
Antivirals that are teratogens
Delavirdine, efavirenz, and ribavirin
antimicrobials
Antivirals associated with neutropenia
Ganciclovir, zidovudine, saquinavir, and interferon
antimicrobials
HIV med used to reduce transmission during birth
AZT (zidovudine)
antimicrobials
Drug used for African sleeping sickness
Suramin
antimicrobials
Drug used in Chagas disease
Nifurtimox
antimicrobials
Cephalosporins able to cross the BBB
Cefixime (2nd) and 3rd generation
antimicrobials
Drug used for N. gonorrhea in females
*Ceftriaxone
antimicrobials
Cephalosporin causes kernicterus in neonates
Ceftriaxone or cefuroxime
antimicrobials
SE of INH
Peripheral neuritis and hepatitis
antimicrobials
Aminoglycoside that is least ototoxic
Streptomycin
antimicrobials
Drug used in exoerythrocytic cycle of malaria
Primaquine
antimicrobials
Oral antibiotic of choice for moderate inflammatory acne
Minocycline
antimicrobials
Drug of choice for leprosy
Dapsone
antimicrobials
DOC for herpes and its MOA
*Acyclovir and inhibits thymidine kinase Acyclovir and inhibits thymidine kinase
antimicrobials
Anti-microbials that cause hemolysis in G6PD-deficient patients
*Sulfonamides
antimicrobials
MOA of erythromycin
Inhibition of protein synthesis at the 50s subunit of ribosome
antimicrobials
Anti-biotic frequently used for chronic UTI prophylaxis
*sulfamethoxazole/ trimethoprim
antimicrobials
Lactam that can be used in PCN allergic patients
Aztreonam
antimicrobials
SE of imipenem
Seizures
antimicrobials
Anti-viral with a dose limiting toxicity of pancreatitis
Didanosine
antimicrobials
Common side effect of hypnotic agents
Sedation
sedative hypnotics
Occurs when sedative hypnotics are used chronically or at high doses
Tolerance
sedative hypnotics
The most common type of drug interaction of sedative hypnotics with other depressant medications
Additive CNS depression
sedative hypnotics
Major effect of benzodiazepines on sleep at high doses
*REM is decreased
benzodiazepines (sedative hypnotic)
Neurologic SE of benzodiazepines
Anterograde amnesia
benzodiazepines (sedative hypnotic)
Reason benzos are used cautiously in pregnancy
*Ability to cross the placenta
benzodiazepines (sedative hypnotic)
Main route of metabolism for benzodiazepines
Hepatic
benzodiazepines (sedative hypnotic)
Benzodiazepine that undergo extrahepatic conjugation (which are useful in older or hepatically impaired)
Lorazepam, oxazepam, and temazepam
benzodiazepines (sedative hypnotic)
MOA for benzodiazepines
increase the FREQUENCY of GABA-mediated chloride ion channel opening
benzodiazepines (sedative hypnotic)
Antidote to benzodiazepine overdose (antagonist that reverses the CNS effects)
*Flumazenil
benzodiazepines (sedative hypnotic)
Benzodiazepine with useful relaxant effects in skeletal muscle spasticity of central origin
Diazepam
benzodiazepines (sedative hypnotic)
Benzodiazepine that has efficacy against absence seizures and in anxiety states, such as agoraphobia
Clonazepam
benzodiazepines (sedative hypnotic)
Benzodiazepines that are the most effective in the treatment of panic disorder
Alprazolam and Clonazepam
benzodiazepines (sedative hypnotic)
Benzodiazepine that is used for anesthesia
Midazolam
benzodiazepines (sedative hypnotic)
DOC for status epilepticus
Diazepam
benzodiazepines (sedative hypnotic)
Longer acting benzodiazepines used in the management of withdrawal states of alcohol and other drugs
Chlordiazepoxide and Diazepam
benzodiazepines (sedative hypnotic)
Agents having active metabolites, long half lives, and a high incidence of adverse effects
Diazepam, Flurazepam, chlordiazepoxide, and clorazepate
benzodiazepines (sedative hypnotic)
Barbiturates may precipitate this hematologic condition
Acute intermittent porphyria
barbituates (sedative hypnotic)
Barbiturates decrease the effectiveness of many other drugs via this pharmacokinetics property
Liver enzyme INDUCTION
barbituates (sedative hypnotic)
Barbiturates MOA
Increase the DURATION of GABA-mediated chloride ion channels
barbituates (sedative hypnotic)
Barbiturate used for the induction of anesthesia
Thiopental
barbituates (sedative hypnotic)
Important drug interaction with chloral hydrate
May displace coumadin from plasma proteins
alcohols (sedative hypnotic)
Site of action for zaleplon and zolpidem
Benzodiazepine receptor BZ1 (although are not considered benzodiazepines)
sedative hypnotics
Good hypnotic activity with less CNS SE than most benzodiazepines
Zolpidem, zaleplon
sedative hypnotics
Agent that is a partial agonist for the 5-HT1A receptor
Buspirone
sedative hypnotics
Drug of choice for generalized anxiety disorder, NOT effective in acute anxiety
Buspirone
sedative hypnotics
Agent that is metabolized to acetaldehyde by alcohol dehydrogenase and microsomal ethanol-oxidizing system (MEOS)
*Ethanol
alcohols
Agent with zero-order kinetics
Ethanol
alcohols
Rate limiting step of alcohol metabolism
Aldehyde dehydrogenase
alcohols
System that increases in activity with chronic exposure and may contribute to tolerance
*MEOS
alcohols
Agent that metabolize acetaldehyde to acetate
Aldehyde dehydrogenase
alcohols
Agents that inhibit alcohol dehydrogenase
Disulfiram, metronidazole, certain sulfonylureas and cephalosporins
alcohols
Agent used in the treatment of alcoholism, if alcohol is consumed concurrently, acetaldehyde builds up and results in nausea, headache, flushing, and hypotension
Disulfiram
alcohols
The most common neurologic abnormality in chronic alcoholics
*Peripheral neuropathy (also excessive alcohol use is associated with HTN, anemia, and MI)
alcohols
Agent that is teratogen and causes a fetal syndrome
Alcohol
alcohols
Agent that is the antidote for methanol overdose
Alcohol
alcohols
Drug that inhibits alcohol dehydrogenase and is used in ethylene glycol exposure
Fomepizole
alcohols
Most frequent route of metabolism
Hepatic enzymes
anti-seizure drugs
Mechanisms of action for Phenytoin, Carbamazepine, Lamotrigine
Sodium blockade
anti-seizure drugs
MOA for benzodiazepines and barbiturates
GABA-related targets
anti-seizure drugs
MOA for Ethosuximide
Calcium channels
anti-seizure drugs
MOA for Valproic acid at high doses
Affect calcium, potassium, and sodium channels
anti-seizure drugs
Drugs of choice for generalized tonic-clonic and partial seizures
*Valproic acid and Phenytoin
anti-seizure drugs
DOC for febrile seizures
Phenobarbital
anti-seizure drugs
Drugs of choice for absence seizures
*Ethosuximide and valproic acid
anti-seizure drugs
Drug of choice for myoclonic seizures
*Valproic acid
anti-seizure drugs
Drugs of choice for status epilepticus
IV diazepam or phenytoin (for prolonged therapy not acute)
anti-seizure drugs
Drugs that can be used for infantile spasms
Corticosteroids
anti-seizure drugs
Anti-seizure drugs used also for bipolar affective disorder (BAD)
Valproic acid, carbamazepine, phenytoin and gabapentin
anti-seizure drugs
Anti-seizure drugs used also for Trigeminal neuralgia
Carbamazepine
anti-seizure drugs
Anti-seizure drugs used also for pain of neuropathic orgin
*Gabapentin
anti-seizure drugs
Anti-seizure agent that exhibits non-linear metabolism, highly protein bound, causes fetal hydantoin syndrome, and stimulates hepatic metabolism
Phenytoin
anti-seizure drugs
SE of phenytoin
*Gingival hyperplasia, nystagmus, diplopia and ataxia
anti-seizure drugs
Anti-seizure agent that induces formation of liver drug-metabolism enzymes, is teratogen and can cause craniofacial anomalies and spina bifida
Carbamazepine
anti-seizure drugs
Agent that inhibits hepatic metabolism, is hepatotoxic and teratogen that can cause neural tube defects and gastrointestinal distress
Valproic acid
anti-seizure drugs
Laboratory value required to be monitored for patients on valproic acid
Serum ammonia and LFT's
anti-seizure drugs
SE for Lamotrigine
Stevens-Johnson syndrome
anti-seizure drugs
SE for Felbamate
Aplastic anemia and acute hepatic failure
anti-seizure drugs
Anti-seizure medication also used in the prevention of migraines
Valproic acid
anti-seizure drugs
Carbamazepine may cause
Agranulocytosis
anti-seizure drugs
Anti-seizure drugs used as alternative drugs for mood stabilization
Carbamazepine, gabapentin, lamotrigine, and valproic acid
anti-seizure drugs
MOA of general anesthetics
Unclear, thought to increase the threshold for firing of CNS neurons
general anesthetics
Inhaled anesthetic with a low blood/gas partition coefficient
Nitrous oxide
general anesthetics
Inversely related to potency of anesthetics
Minimum alveolar anesthetic concentration (MAC)
general anesthetics
Inhaled anesthetics metabolized by liver enzymes which has a major role in the toxicity of these agents
Halothane and methoxyflurane
general anesthetics
Most inhaled anesthetics SE
Decrease arterial blood pressure
general anesthetics
Inhaled anesthetics are myocardial depressants
Enflurane and halothane
general anesthetics
Inhaled anesthetic causes peripheral vasodilation
Isoflurane
general anesthetics
Inhaled anesthetic that may sensitize the myocardium to arrhythmogenic effects of catecholamines and has produced hepatitis
Halothane
general anesthetics
Inhaled anesthetics, less likely to lower blood pressure than other agents, and has the smallest effect on respiration
Nitrous oxide
general anesthetics
Fluoride released by metabolism of this inhaled anesthetic may cause renal insufficiency
Methoxyflurane
general anesthetics
Prolonged exposure to this inhaled anesthetic may lead to megaloblastic anemia
Nitrous oxide
general anesthetics
Pungent inhaled anesthetic which leads to high incidence of coughing and vasospasm
Desflurane
general anesthetics
DOC for malignant hyperthermia that may be caused by use of halogenated anesthetics
*Dantrolene
general anesthetics
IV barbiturate used as a pre-op anesthetic
Thiopental
general anesthetics
Benzodiazepine used adjunctively in anesthesia
Midazolam
general anesthetics
Benzodiazepine receptor antagonist, it accelerates recovery from benzodiazepine overdose
*Flumazenil
general anesthetics
This produces "dissociative anesthesia", is a cardiovascular stimulant which may increases intracranial pressure, and hallucinations occur during recovery
Ketamine
general anesthetics
Opioid associated with respiratory depression, but is used in high risk patients who may not survive full general anesthetia
*Fentanyl
general anesthetics
State of analgesia and amnesia produced when fentanyl is used with droperidol and nitrous oxide
Neuroleptanesthesia
general anesthetics
Produces both rapid anesthesia and recovery, has antiemetic activity and commonly used for outpatient surgery, may cause marked hypotension
Propofol
general anesthetics
MOA of local anesthetics (LA's)
Block voltage-dependent sodium channels
local anesthetics
This may enhance activity of local anesthetics
Hyperkalemia
local anesthetics
This may antagonize activity of local anesthetics
Hypercalcemia
local anesthetics
Almost all local anesthetics have this property and sometimes require the administration of vasoconstrictors (ex. Epinephrine) to prolong activity
Vasodilation
local anesthetics
Local anesthetic with vasoconstrictive property, favored for head, neck, and pharyngeal surgery
Cocaine
local anesthetics
Longer acting local anesthetics which are less dependent on vasoconstrictors
Tetracaine and bupivacaine
local anesthetics
These LA's have surface activity
Cocaine and benzocaine
local anesthetics
Most important toxic effects of most local anesthetics
CNS toxicity
local anesthetics
Commonly abused LA which has cardiovascular toxicity including severe hypertension with cerebral hemorrhage, cardiac arrhythmias, and myocardial infarction
Cocaine
local anesthetics
LA causing methemoglobinemia
Prilocaine
local anesthetics
Structurally related to acetylcholine, used to produce muscle paralysis in order to facilitate surgery or artifical ventilation. Full doses lead to respiratory paralysis and require ventilation
Neuromuscular blocking drugs
local anesthetics
These drugs strongly potentiate and prolong effect of neuromuscular blockade (NMB)
Inhaled anesthetics, especially isoflurane, aminoglycosides, and antiarrhythmic
local anesthetics
These prevent the action of Ach at the skeletal muscle endplate to produce a "surmountable blockade," effect is reversed by cholinesterase inhibitors (ex. neostigmine or pyridostigmine)
Nondepolarizing type antagonists
local anesthetics
Agent with long duration of action and is sost likely to cause histamine release
Tubocurarine
local anesthetics
Non-depolarizing antagonist has short duration
Mivacurium
local anesthetics
Agent can blocking muscarinic receptors
Pancuronium
local anesthetics
Agent undergoing Hofmann elimination (breaking down spontaneously)
Atracurium
local anesthetics
One depolarizing blocker that causes continuous depolarization and results in muscle relaxation and paralysis, xcuses muscle pain postoperatively and myoglobinuria may occur
Succinylcholine
local anesthetics
During Phase I these agents worsen the paralysis by succinylcholine, but during phase II they reverse the blockade produced by succinylcholine
Cholinesterase inhibitors
local anesthetics
Agents acting in the CNS or in the skeletal muscle, used to reduce abnormally elevated tone caused by neurologic or muscle end plate disease
Spasmolytic drugs
spasmolytic drugs
Facilitates GABA presynaptic inhibition
Diazepam
spasmolytic drugs
GABA agonist in the spinal cord
Baclofen
spasmolytic drugs
Similar to clonidine and may cause hypotension
Tizanidine
spasmolytic drugs
DOC for malignant hyperthermia by acting on the sacroplasmic reticulum or skeletal muscle
*Dantrolene
spasmolytic drugs
Agent used for acute muscle spasm
Cyclobenzaprine
spasmolytic drugs
Antipsychotics, reserpine at high doses, and MPTP (by-product of illicit meperidine analog) and is irreversible
*Drug induced Parkinsonism
drugs used in parkinsonism and other movement d/o
Agent used in drug therapy of Parkinson's instead of Dopamine which has low bioavailability and does not cross the BBB
L-dopa
drugs used in parkinsonism and other movement d/o
This is combined with L-dopa, inhibits DOPA decarboxylase (active only peripherally) which allows lower effective doses of L-dopa and allows for fewer SE's (GI distress, postural hypotension, and dyskinesias)
Carbidopa
drugs used in parkinsonism and other movement d/o
Clinical response that may fluctuate in tx of Parkinson's dx
"On-off-phenomenon"
drugs used in parkinsonism and other movement d/o
Anti-Parkinson's drug which increases intraocular pressure and is contraindicated in closed angle glaucoma
Levodopa
drugs used in parkinsonism and other movement d/o
Ergot alkaloid that is a partial agonist at D2 receptors in the brain, used for patients who are refractory or cannot tolerate levodopa, causes erythromelalgia
Bromocriptine
drugs used in parkinsonism and other movement d/o
Non ergot agents used as first-line therapy in the initial management of Parkinson's
Pramipexole and ropinirole
drugs used in parkinsonism and other movement d/o
Enhances dopaminergic neurotransmission SE's include CNS excitation, acute toxic psychosis and livedo reticularis
Amantadine
drugs used in parkinsonism and other movement d/o
Inhibitor of MAO type B which metabolizes dopamine, used adjunct to levodopa or as sole agent in newly diagnosed pt's
Selegiline
drugs used in parkinsonism and other movement d/o
Inhibitors of catechol-O-methyltransferase (COMT), used as adjuncts in Parkinson's dx and cause acute hepatic failure (monitor LFT's)
Entacapone and Tolcapone
drugs used in parkinsonism and other movement d/o
Agent decreases the excitatory actions of cholinergic neurons. May improve tremor and rigidity but have LITTLE effect on bradykinesia. Atropine-like side effects
Benztropine
drugs used in parkinsonism and other movement d/o
Agent effective in physiologic and essential tremor
Propranolol
drugs used in parkinsonism and other movement d/o
Agents used in Huntington's Disease
Tetrabenazine (amine depleting drug), Haloperidol (antipsychotic)
drugs used in parkinsonism and other movement d/o
Agents used in Tourette's dx
Haloperidol or pimozide
drugs used in parkinsonism and other movement d/o
Chelating agent used in Wilson's disease
Penicillamine
drugs used in parkinsonism and other movement d/o
Extrapyramidal dysfunction is more common with these agents, which block this subtype of dopamine receptor
Older antipsychotic agents, D2 receptors
antipsychotics
Side effects occuring in antipsychotics that block dopamine
*Hyperprolactinemia, menorrhea, galactorrhea, confusion, mood changes, decreased sexual interest, and weight gain
antipsychotics
Antipsychotics that reduce positive symptoms only
Older antipsychotics
antipsychotics
Newer atypical antipsychotics that also improve some of the negative symptoms and help acute agitation
Olanzapine, aripiprazole, and sertindole
antipsychotics
Antipsychotic used in the treatment of psychiatric symptoms in patients with dementia
*Risperidone
antipsychotics
Atypical antipsychotic causing high prolactin levels
*Risperidone
antipsychotics
Newer atypical antipsychotic used for bipolar disorder, known to cause weight gain, and adversely affect diabetes
Olanzapine
antipsychotics
Agent more frequently associated with extrapyramidal side effects that can be treated with benzodiazepine, diphenhydramine or muscarinic blocker
Haloperidol
antipsychotics
Drug used in neuroleptic malignant syndrome
*Dantrolene
antipsychotics
Agents may exacerbate tardive dyskinesias (may be irreversible and there is no treatment)
Muscarinic blockers
antipsychotics
Antipsychotic having the strongest autonomic effects
*Thioridazine
antipsychotics
Antipsychotic having the weakest autonomic effects
Haloperidol
antipsychotics
Antipsychotic that does not block muscarinic or histamine receptors, and it prolongs the QT interval
Sertindole
antipsychotics
Only phenothiazine not exerting antiemetic effects, can cause visual impairment due to retinal deposits, and high doses have been associated with ventricular arrhythmias
Thioridazine
antipsychotics
Agent having no effect on D2 receptors, blocks D4, reserved for resistant schizophrenia, and can cause agranulocytosis
*Clozapine
antipsychotics
Anti-psychotic not shown to cause tardive dyskinesia
*Clozapine
antipsychotics
Anti-psychotics available in depot preparation
Fluphenazine and haloperidol
antipsychotics
Reduced seizure threshold
Low-potency typical antipsychotics and clozapine
antipsychotics
Orthostatic hypotension and QT prolongation
Low potency and risperidone
antipsychotics
Increased risk of developing cataracts
Quetiapine
antipsychotics
Major route of elimination for Lithium
*Kidneys
lithium
Patients being treated with lithium, who are dehydrated, or taking diuretics concurrently, could develop
*Lithium toxicity
lithium
Drug increases the renal clearance hence decreases levels of lithium
Theophylline
lithium
Lithium is associated with this congenital defect
Cardiac anomalies and is contraindicated in pregnancy or lactation
lithium
DOC for bipolar affective disorder
*Lithium
lithium
SE of lithium
*Tremor, sedation, ataxia, aphasia, thyroid enlargement, and reversible diabetes insipidus
lithium
Example of three antidepressants that are indicated for obsessive compulsive disorder
Clomipramine, fluoxetine and fluvoxamine
antidepressants
Neurotransmitters affected by the action of antidepressants
Norepinephrine and serotonin
antidepressants
Usual time needed for full effect of antidepressant therapy
2 to 3 weeks
antidepressants
Population group especially sensitive to side effects of antidepressants
Elderly patients
antidepressants
All antidepressants have roughly the same efficacy in treating depression, agents are chosen based on these criterion
Side-effect profile and prior pt response
antidepressants
Well-tolerated and are first-line antidepressants
SSRI's, bupropion, and venlafaxine
antidepressants
Most useful in patients with significant anxiety, phobic features, hypochondriasis, and resistant depression
Monamine oxidase inhibitors
MAOIs (antidepressants)
Condition will result from in combination of MAOI with tyramine containing foods (ex. wine, cheese, and pickled meats)
Hypertensive crisis
MAOIs (antidepressants)
MAOI should not be administered with SSRI's or potent TCA's due to development of this condition
Serotonin syndrome
MAOIs (antidepressants)
Sedation is a common side effect of these drugs, they lower seizure threshold, uses include BAD, acute panic attacks, phobias, enuresis, and chronic pain and their overdose can be deadly
Tricyclic antidepressants (TCA)
TCAs (antidepressants)
Three C's associated with TCA toxicity
Coma, Convulsions, Cardiac problems (arrhythmias and wide QRS)
TCAs (antidepressants)
Agents having higher sedation and antimuscarinic effects than other TCA's
Tertiary amines
TCAs (antidepressants)
TCA used in chronic pain, a hypnotic, and has marked antimuscarinic effects
Amitriptyline
TCAs (antidepressants)
TCA used in chronic pain, enuresis, and ADD
*Imipramine
TCAs (antidepressants)
TCA with greatest sedation of this group, and marked antimuscarinic effects, used for sleep
Doxepin
TCAs (antidepressants)
TCA used in obsessive compulsive disorder (OCD), most significant of TCA's for risk of seizure, weight gain, and neuropsychiatric signs and symptoms
Clomipramine
TCAs (antidepressants)
Secondary amines that have less sedation and more excitation effect
Nortriptyline, Desipramine
TCAs (antidepressants)
Antidepressant associated with neuroleptic malignant syndrome
Amoxapine
heterocyclics (antidepressants)
Antidepressant associated with seizures and cardiotoxicity
Maprotiline
heterocyclics (antidepressants)
Antidepressant having stimulant effects similar to SSRI's and can increase blood pressure
Venlafaxine
heterocyclics (antidepressants)
Antidepressant inhibiting norepinephrine, serotonin, and dopamine reuptake
Venlafaxine
heterocyclics (antidepressants)
Antidepressant also used for sleep that causes priapism
Trazodone
heterocyclics (antidepressants)
Antidepressant which is inhibitor of CYP450 enzymes and may be associated with hepatic failure
Nefazodone
heterocyclics (antidepressants)
Heterocyclic antidepressants least likely to affect sexual performance, used for management of nicotine withdrawal, SE's include dizziness, dry mouth, aggravation of psychosis, and seizures
*Bupropion
heterocyclics (antidepressants)
Antidepressant with MOA as alpha 2 antagonist, has effects on both 5-HT and NE, blocks histamine receptors, and is sedating
Mirtazapine
heterocyclics (antidepressants)
SE of mirtazapine
Liver toxicity, increased serum cholesterol
heterocyclics (antidepressants)
Except for these agents all SSRI have significant inhibition of CytP450 enzymes
Citalopram and its metabolite escitalopram
SSRIs (antidepressants)
SSRI with long T1/2 and can be administered once weekly for maintenance, not acute tx
Fluoxetine
SSRIs (antidepressants)
SSRI indicated for premenstrual dysphoric disorder
Fluoxetine (Sarafem)
SSRIs (antidepressants)
Some of SSRIs' therapeutic effects beside depression
Panic attacks, social phobias, bulimia nervosa, and PMDD premenstrual dysphoric disorder), OCD
SSRIs (antidepressants)
SSRI's less likely to cause a withdrawal syndrome
Fluoxetine
SSRIs (antidepressants)
Inhibit synaptic activity of primary afferents and spinal cord pain transmission neurons
Ascending pathways
Opiod Analgesics and Antagonists
Activation of these receptors close Ca2+ ion channels to inhibit neurotransmitter release
*Presynaptic mu, delta, and kappa receptors
Opiod Analgesics and Antagonists
Activation of these receptors open K+ ion channels to cause membrane hyperpolarization
Postsynaptic Mu receptors
Opiod Analgesics and Antagonists
Tolerance to all effects of opioid agonists can develop except
*Miosis and constipation
Opiod Analgesics and Antagonists
All opioids except this agent (which has a muscarinic blocking action) cause pupillary constriction
Meperidine
Opiod Analgesics and Antagonists
SE of these drugs include dependence, withdrawal syndrome, sedation, euphoria, respiratory depression nausea and vomiting, constipation, biliary spasm, increased ureteral and bladder tone, and reduction in uterine tone
Opioid Analgesics
Opiod Analgesics and Antagonists
Strong opioid agonists
Morphine, methadone, meperidine, and fentanyl
Opiod Analgesics and Antagonists
Opioids used in anesthesia
Morphine and fentanyl
Opiod Analgesics and Antagonists
Opioid used in the management of withdrawal states
*Methadone
Opiod Analgesics and Antagonists
Opioid available trans-dermally
*Fentanyl
Opiod Analgesics and Antagonists
Opioid that can be given PO, by epidural, and IV, which helps to relieve the dyspnea of pulmonary edema
*Morphine
Opiod Analgesics and Antagonists
Use of this opioid with MAOI can lead to hyperpyrexic coma, and with SSRI's can lead to serotonin syndrome
Meperidine
Opiod Analgesics and Antagonists
Moderate opioid agonists
*Codeine, hydrocodone, and oxycodone
Opiod Analgesics and Antagonists
Weak opioid agonist, poor analgesic, its overdose can cause severe toxicity including respiratory depression, circulatory collapse, pulmonary edema, and seizures
Propoxyphene
Opiod Analgesics and Antagonists
Partial opioid agonist, considered a strong analgesic, has a long duration of action and is resistant to naloxone reversal
Buprenorphine
Opiod Analgesics and Antagonists
Opioid antagonist that is given IV and had short DOA
*Naloxone
Opiod Analgesics and Antagonists
Opioid antagonist that is given orally in alcohol dependency programs
*Naltrexone
Opiod Analgesics and Antagonists
These agents are used as antitussive
Dextromethorphan, Codeine
Opiod Analgesics and Antagonists
These agents are used as antidiarrheal
Diphenoxylate, Loperamide
Opiod Analgesics and Antagonists
Inhalant anesthetics
NO, chloroform, and diethyl ether
Drugs of Abuse
Toxic to the liver, kidney, lungs, bone marrow, peripheral nerves, and cause brain damage in animals, sudden death has occurred following inhalation
Fluorocarbons and Industrial solvents
Drugs of Abuse
Cause dizziness, tachycardia, hypotension, and flushing
Organic nitrites
Drugs of Abuse
Causes acne, premature closure of epiphyses, masculinization in females, hepatic dysfunction, MI, and increases in libido and aggression
Steroids
Drugs of Abuse
Readily detected markers that may assist in diagnosis of the cause of a drug overdose include
*Changes in heart rate, blood pressure, respiration, body temperature, sweating, bowel signs, and pupillary responses
Drugs of Abuse
Most commonly abused in health care professionals
Heroin, morphine, oxycodone, meperidine and fentanyl
Drugs of Abuse
This route is associated with rapid tolerance and psychologic dependence
IV administration
Drugs of Abuse
Leads to respiratory depression progressing to coma and death
*Overdose of opioids
Drugs of Abuse
Lacrimation, rhinorrhea, yawning, sweating, weakness, gooseflesh, nausea, and vomiting, tremor, muscle jerks, and hyperpnea are signs of this syndrome
Abstinence syndrome
Drugs of Abuse
Treatment for opioid addiction
Methadone, followed by slow dose reduction
Drugs of Abuse
This agent may cause more severe, rapid and intense symptoms to a recovering addict
*Naloxone
Drugs of Abuse
Sedative-Hypnotics action
Reduce inhibition, suppress anxiety, and produce relaxation
Drugs of Abuse
Additive effects when Sedative-Hypnotics used in combination with these agents
CNS depressants
Drugs of Abuse
Common mechanism by which overdose result in death
Depression of medullary and cardiovascular centers
Drugs of Abuse
"Date rape drug"
*Flunitrazepam (rohypnol)
Drugs of Abuse
The most important sign of withdrawal syndrome
Excessive CNS stimulation (seizures)
Drugs of Abuse
Treatment of withdrawal syndrome involves
Long-acting sedative-hypnotic or a gradual reduction of dose, clonidine or propranolol
Drugs of Abuse
These agents are CNS depressants
*Ethanol, Barbiturates, and Benzodiazepines
Drugs of Abuse
Withdrawal from this drug causes lethargy, irritability, and headache
Caffeine
Drugs of Abuse
W/D from this drug causes anxiety and mental discomfort
Nicotine
Drugs of Abuse
Treatments available for nicotine addiction
*Patches, gum, nasal spray, psychotherapy, and bupropion
Drugs of Abuse
Chronic high dose abuse of nicotine leads to
Psychotic state, overdose causes agitation, restlessness, tachycardia, hyperthermia, hyperreflexia, and seizures
Drugs of Abuse
Tolerance is marked and abstinence syndrome occurs
Amphetamines
Drugs of Abuse
Amphetamine agents
Dextroamphetamines and methamphetamine
Drugs of Abuse
These agents are congeners of Amphetamine
DOM, STP, MDA, and MDMA "ecstasy"
Drugs of Abuse
Overdoses of this agent with powerful vasoconstrictive action may result in fatalities from arrhythmias, seizures, respiratory depression, or severe HTN (MI and stroke)
Cocaine "super-speed"
Drugs of Abuse
Most dangerous of the currently popular hallucinogenic drugs, OD leads to nystagmus, marked hypertension, and seizures, presence of both horizontal and vertical nystagmus is pathognomonic
PCP
Drugs of Abuse
Removal of PCP may be aided
Urinary acidification and activated charcoal or continual nasogastric suction
Drugs of Abuse
THC is active ingredient, SE's include impairment of judgment, and reflexes, decreases in blood pressure and psychomotor performance occur
*Marijuana
Drugs of Abuse
This agent has greater affinity for muscarinic receptors and used for postoperative and neurogenic ileus and urinary retention
*Bethanechol
Direct Acting (Cholinoreceptor-Activatin & Cholinesterase-Inhibiting Drugs)
Only direct acting agent that is very lipid soluble and used in glaucoma
Pilocarpine
Direct Acting (Cholinoreceptor-Activatin & Cholinesterase-Inhibiting Drugs)
This agent used to treat dry mouth in Sjögren's syndrome
Cevimeline
Direct Acting (Cholinoreceptor-Activatin & Cholinesterase-Inhibiting Drugs)
Indirect-Acting ACh Agonist, alcohol, short DOA and used in diagnosis of myasthenia gravis
Edrophonium
Direct Acting (Cholinoreceptor-Activatin & Cholinesterase-Inhibiting Drugs)
Carbamate with intermediate action postoperative and neurogenic ileus and urinary retention
Neostigmine
Direct Acting (Cholinoreceptor-Activatin & Cholinesterase-Inhibiting Drugs)
Treatment of atropine overdose and glaucoma (because lipid soluable). Enters the CNS rapidly and has a stimulant effect, which may lead to convulsions
Physostigmine
Direct Acting (Cholinoreceptor-Activatin & Cholinesterase-Inhibiting Drugs)
Treatment of myasthenia gravis
Pyridostigmine
Direct Acting (Cholinoreceptor-Activatin & Cholinesterase-Inhibiting Drugs)
Antiglaucoma organophosphate
Echothiophate
Organophosphates (Cholinoreceptor-Activatin & Cholinesterase-Inhibiting Drugs)
Associated with an increased incidence of cataracts in patients treated for glaucoma
Long acting cholinesterase inhibitors
Organophosphates (Cholinoreceptor-Activatin & Cholinesterase-Inhibiting Drugs)
Scabicide organophosphate
Malathion
Organophosphates (Cholinoreceptor-Activatin & Cholinesterase-Inhibiting Drugs)
Organophosphate anthelmintic agent with long DOA
Metrifonate
Organophosphates (Cholinoreceptor-Activatin & Cholinesterase-Inhibiting Drugs)
Toxicity of organophosphate:
*DUMBELSS (diarrhea, urination, miosis, bronchoconstriction, excitation of skeletal muscle and CNS, lacrimation, salivation, and sweating)
Organophosphates (Cholinoreceptor-Activatin & Cholinesterase-Inhibiting Drugs)
The most important cause of acute deaths in cholinesterase inhibitor toxicity
Respiratory failure
Organophosphates (Cholinoreceptor-Activatin & Cholinesterase-Inhibiting Drugs)
The most toxic organophosphate
Parathion
Organophosphates (Cholinoreceptor-Activatin & Cholinesterase-Inhibiting Drugs)
Treatment of choice for organophosphate overdose
Atropine
Organophosphates (Cholinoreceptor-Activatin & Cholinesterase-Inhibiting Drugs)
This agent regenerates active cholinesterase and is a chemical antagonist used to treat organophosphate exposure
Pralidoxime
Organophosphates (Cholinoreceptor-Activatin & Cholinesterase-Inhibiting Drugs)
Prototypical drug is atropine
Nonselective Muscarinic Antagonists
Cholinoreceptor Blockers & Cholinesterase Regenerators
Treat manifestations of Parkinson's disease and EPS
*Benztropine, trihexyphenidyl
Cholinoreceptor Blockers & Cholinesterase Regenerators
Treatment of motion sickness
*Scopolamine
Cholinoreceptor Blockers & Cholinesterase Regenerators
Produce mydriasis and cycloplegia
*Atropine, homatropine tropicamide
Cholinoreceptor Blockers & Cholinesterase Regenerators
Bronchodilation in asthma and COPD
*Ipratropium
Cholinoreceptor Blockers & Cholinesterase Regenerators
Reduce transient hyper GI motility
Dicyclomine, methscopolamine
Cholinoreceptor Blockers & Cholinesterase Regenerators
Cystitis, postoperative bladder spasms, or incontinence
Oxybutynin, dicyclomine
Cholinoreceptor Blockers & Cholinesterase Regenerators
Toxicity of anticholinergics
block SLUD (salivation, lacrimation, urination, defecation
Cholinoreceptor Blockers & Cholinesterase Regenerators
Another pneumonic for anticholinergic toxicity
"dry as a bone, red as a beet, mad as a hatter, hot as a hare, blind as a bat"
Cholinoreceptor Blockers & Cholinesterase Regenerators
Atropine fever is the most dangerous effect and can be lethal in this population group
Infants
Cholinoreceptor Blockers & Cholinesterase Regenerators
Contraindications to use of atropine
Infants, closed angle glaucoma, prostatic hypertrophy
Cholinoreceptor Blockers & Cholinesterase Regenerators
Prototype ganglion blocker
Hexamethonium
Nicotinic Antagonists
Limiting adverse effect of ganglion blockade that patients usually are unable to tolerate
Severe hypertension
Nicotinic Antagonists
Reversal of blockade by neuromuscular blockers
Cholinesterase inhibitors
Nicotinic Antagonists
Tubocurarine is the prototype, pancuronium, atracurium, vecuronium are newer short acting agent, produce competitive block at end plate nicotinic receptor, causing flaccid paralysis
Nondepolarizing Neuromuscular Blockers
Nicotinic Antagonists
Only member of depolarizing neuromuscular blocker, causes fasciculation during induction and muscle pain after use
Succinylcholine
Nicotinic Antagonists
Chemical antagonists that bind to the inhibitor of ACh Estrace and displace the enzyme (if aging has not occurred)
Cholinesterase Regenerators
Nicotinic Antagonists
Used to treat patients exposed to insecticides such as parathion
Pralidoxime
Nicotinic Antagonists
Pneumonic for beta receptors
*You have 1 heart (Beta 1) and 2 lungs (Beta 2)
Sympathomimetics
This is the drug of choice for anaphylactic shock
*Epinephrine
Sympathomimetics
Phenylisopropylamines that are used legitimately and abused for narcolepsy, attention deficit disorder, and weight reduction
Amphetamines
Sympathomimetics
Alpha agonist used to produce mydriasis and reduce conjunctival itching and congestion caused by irritation or allergy, it does not cause cycloplegia
Phenylephrine
Sympathomimetics
Epinephrine and dipivefrin are used for
Glaucoma
Sympathomimetics
Newer alpha 2 agonist (apraclonidine and brimonidine) treat glaucoma
Reduce aqueous synthesis
Sympathomimetics
Short acting Beta 2 agonists that is drug of choice in treatment of acute asthma but not recommended for prophylaxis
Albuterol
Sympathomimetics
Longer acting Beta 2 agonists is recommended for prophylaxis of asthma
Salmeterol
Sympathomimetics
These agents increase blood flow and may be beneficial in treatment of acute heart failure and some types of shock
Beta1 agonists
Sympathomimetics
These agents decrease blood flow or increase blood pressure, are local decongestant, and used in therapy of spinal shock (temporary maintenance of blood pressure which may help maintain perfusion
*Alpha1 agonists
Sympathomimetics
Shock due to septicemia or myocardial infarction is made worse by
Increasing afterload and tissue perfusion declines
Sympathomimetics
Often mixed with local anesthetic to
Reduce the loss from area of injection
Sympathomimetics
Chronic orthostatic hypotension can be treated with
Midodrine
Sympathomimetics
Beta 2 agonist used to suppress premature labor, but cardiac stimulatory effects may be hazardous to mother and fetus
Terbutaline
Sympathomimetics
Long acting sympathomimetic, sometimes used to improve urinary continence in children and elderly with enuresis
Ephedrine
Sympathomimetics
Alpha 1 agonist toxicity
*Hypertension
Sympathomimetics
Beta 1 agonist toxicity
Sinus tachycardia and serious arrhythmias
Sympathomimetics
Beta 2 agonist toxicity
Skeletal muscle tremor
Sympathomimetics
The selective agents loose their selectivity at
high doses
Sympathomimetics
Nonselective alpha-blocking drug, long acting and irreversible, and used to treat pheochromocytoma. Blocks 5-HT, so occasionaly used for carcinoid tumor. Blocks H1 and used in mastocytosis
Phenoxybenzamine
Adenoceptor Blocker
Nonselective alpha-blocking drug, short acting and reversible, used for rebound HTN from rapid clonidine withdrawal, and Raynaud's phenomena
Phentolamine
Adenoceptor Blocker
Selective Alpha 1 blocker used for hypertension, BPH, may cause first dose orthostatic hypotension
*Prazosin, terazosin, doxazosin
Adenoceptor Blocker
Selective Alpha 2 blocker used for impotence (controversial effectiveness)
Yohimbine
Adenoceptor Blocker
SelectiveB1 Receptor blockers that may be useful in treating patients with asthma
*Acebutolol, atenolol, esmolol, metoprolol
Adenoceptor Blocker
Combined alpha and beta blocking agents that may have application in treatment of CHF
Labetalol and carvedilol
Adenoceptor Blocker
Beta blockers partial agonist activity (intrinsic sympathomimetic activity) cause some bronchodilation and may have an advantage in treating patients with asthma
Pindolol and acebutolol
Adenoceptor Blocker
This beta blocker lacks local anesthetic activity (decreases protective reflexes and increases the risk of corneal ulceration) and used in treating glaucoma
*Timolol
Adenoceptor Blocker
This parenteral beta blocker is a short acting
Esmolol
Adenoceptor Blocker
This beta blocker is the longest acting
Nadolol
Adenoceptor Blocker
These beta blockers are less lipid soluble
Acebutolol and atenolol
Adenoceptor Blocker
This beta blocker is highly lipid soluble and may account for side effects such as nightmares
Propranolol
Adenoceptor Blocker
Clinical uses of these agents include treatment of HTN, angina, arrhythmias, and chronic CHF
Beta blockers
Adenoceptor Blocker
Toxicity of these agents include bradycardia, AV blockade, exacerbation of acute CHF, signs of hypoglycemia may be masked (tachycardia, tremor, and anxiety)
Beta blockers
Adenoceptor Blocker
Cholinomimetics that increase outflow, open trabecular meshwork, and cause ciliary muscle contraction
Pilocarpine, carbachol, physostigmine
Glaucoma (all agents except diuretics)
Nonselective alpha agonists that increases outflow, probably via the uveoscleral veins
Epinephrine, dipivefrin
Glaucoma (all agents except diuretics)
Selective alpha agonists that decreases aqueous secretion
Apraclonidine, brimonidine
Glaucoma (all agents except diuretics)
These Beta blockers decrease aqueous secretion
*Timolol (nonselective), betaxolol (selective)
Glaucoma (all agents except diuretics)
This diuretic decreases aqueous secretion due to lack of HCO3- ion. Causes drowsiness and paresthesias, alkalinization of the urine may precipitate calcium salts, hypokalemia, acidosis
Acetazolamide
Glaucoma (all agents except diuretics)
This agent cause increased aqueous outflow
Prostaglandin PGF2a
Glaucoma (all agents except diuretics)
Inhibit angiotensin-converting enzyme (ACE)
*Ace inhibitors
Antihypertensives
Captopril and enalapril (-OPRIL ending) are
*Ace inhibitors
Antihypertensives
SE of ACE inhibitors
*Dry cough, hyperkalemia
Antihypertensives
Ace inhibitors are contraindicated in
*pregnancy and with K+
Antihypertensives
Losartan and valsartan block
*Angiotensin receptor
Antihypertensives
Angiotensin receptor blockers do NOT cause
*Dry cough
Antihypertensives
Block L-type calcium channel
Calcium channel blockers
Antihypertensives
CCB contraindicated in CHF
*Verapamil
Antihypertensives
CCB with predominate effect on arteriole dilation
Nifedipine
Antihypertensives
SE of CCB
*Constipation, edema, and headache
Antihypertensives
Reduce heart rate, contractility, and O2 demand
*Beta-blockers
Antihypertensives
B-blockers that are more cardioselective
Beta C2001-selective blockers
Antihypertensives
Cardioselective Beta 1-blockers
*Atenolol, acebutolol, and metoprolol
Antihypertensives
Beta-blockers should be used cautiously in
Asthma (bronchospastic effects), diabetes (block signs of hypoglycemia) and peripheral vascular disease
Antihypertensives
Non-selective Beta-blocker also used for migraine prophylaxis
Propranolol
Antihypertensives
SE of beta blockers
*Bradycardia, SEXUAL DYSFUNCTION, decrease in HDL, and increase in Triglycerols (TG)
Antihypertensives
Alpha 1selective blockers
*Prazosin, terazosin and doxazosin (-AZOSIN ending)
Antihypertensives
Non-selective Alpha1blockers use to treat pheochromocytoma
Phenoxybenzamine
Antihypertensives
For rebound HTN from rapid clonidine withdrawal
Phentolamine
Antihypertensives
A1a-selective blocker used for BPH
*Tamsulosin (Flomax)
Antihypertensives
SE of alpha blockers
*Orthostatic hypotension (especially with first dose) and reflex tachycardia
Antihypertensives
Presynaptic Alpha 2 agonist used in HTN
Clonidine, and methyldopa
Antihypertensives
SE of methyldopa
Positive Comb's test, depression
Antihypertensives
Methyldopa is contraindicated in
*Geriatrics due to its CNS (depression) effects
Antihypertensives
SE of clonidine
Rebound HTN, sedation, dry mouth
Antihypertensives
Ganglionic blockers formerly used in HTN
Trimethaphan, and hexamethonium
Antihypertensives
Direct vasodilator of arteriolar smooth muscle
Hydralazine
Antihypertensives
SE of hydralazine
*Lupus-like syndrome
Antihypertensives
Arterial vasodilator that works by opening K+ channels
Minoxidil
Antihypertensives
SE of minoxidil
Hypertrichosis
Antihypertensives
IV Drug used Hypertensive Crisis
Nitroprusside
Antihypertensives
Nitroprusside vasodilates
Arteries and veins
Antihypertensives
Toxicity caused by nitroprusside and treatment
Cyanide toxicity treated with sodium thiosulfate
Antihypertensives
Carbonic anhydrase inhibitor
Acetazolamide
Diuretics
Diuretic used for mountain sickness and glaucoma
*Acetazolamide
Diuretics
SE of acetazolamide
*Paresthesias, alkalization of the urine (which may ppt. Ca salts), hypokalemia, acidosis, and encephalopathy in patients with hepatic impairment
Diuretics
MOA of loop diuretics
inhibits Na+/K+/2Cl- cotransport
Diuretics
Site of action of loop diuretics
*Thick ascending limb
Diuretics
SE of loop (furosemide) diuretics
*Hyperuricemia, hypokalemia and ototoxicity
Diuretics
Aminoglycosides used with loop diuretics potentiate adverse effect
Ototoxicity
Diuretics
Loops lose and thiazide diuretics retain
*Calcium
Diuretics
MOA of thiazide diuretics
Inhibit Na+/Cl- cotransport
Diuretics
Site of action of thiazide diuretics
*Work at early distal convoluted tubule
Diuretics
Class of drugs that may cause cross-sensitivity with thiazide diuretics
Sulfonamides
Diuretics
SE of thiazide (HCTZ) diuretics
*Hyperuricemia, hypokalemia and hyperglycemia
Diuretics
Potassium sparing diuretics inhibit
*Na+/K+ exchange
Diuretics
Diuretic used to treat primary aldosteronism
*Spironolactone
Diuretics
SE of spironolactone
*Gynecomastia hyperkalemia, and impotence
Diuretics
Osmotic diuretic used for increased intracranial pressure
*Mannitol
Diuretics
ADH agonist used for pituitary diabetes insipidus
*Desmopressin (DDAVP)
ADH agonist and antagonists
Used for SIADH
Demeclocycline
ADH agonist and antagonists
SE of demeclocycline
Bone marrow and teeth discoloration for children under 8 years of age
ADH agonist and antagonists
MOA of class I A (eg. Procainamide), class IB (eg. Lidocaine), and class IC (eg. Flecainide) antiarrhythmics
*Sodium channel blockers
Antiarrhythmic Agents
SE of procainamide
*Lupus-like syndrome
Antiarrhythmic Agents
Limiting side effect of Quinidine
*Prolongs QT interval
Antiarrhythmic Agents
Other side effects of Quinidine
Thrombocytopenic purpura, and CINCHONISM
Antiarrhythmic Agents
Major drug interaction with Quinidine
Increases concentration of Digoxin
Antiarrhythmic Agents
DOC for management of acute Ventricular arrhythmias
*Lidocaine
Antiarrhythmic Agents
DOC for digoxin induced arrhythmias
Phenytoin
Antiarrhythmic Agents
SE of phenytoin
Gingival hyperplasia
Antiarrhythmic Agents
Class of anti-arrhythmics that has a pro-arrhythmic effect (CAST trial), therefore are used as last line agents
Class IC (flecainide, propafenone, moricizine)
Antiarrhythmic Agents
Class II antiarrhythmics are
B-blockers
Antiarrhythmic Agents