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22 Cards in this Set

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Muscarinic Antagonist Prototypes
Atropine is the prototype that doesn't cross the BBB until high doses are reached.
Scopolamine is similar, comes from the same plant but readily enters the CNS
Scopolamine
Systemically it will enter the CNS and cause amnesia/sedation. Medically it is used in patch form to prevent motion sickness
Homatropine and Tropicomide
Atropine derivatives with shorter duration. - Used to dilate the pupil
Ipratropium and tiotropium
I for inhaled - Quat-amines - not orally absorbed and don't cross BBB. Inhaled for asthma/COPD
Atropine + Diphenoxylate
Atropine slows down your GI tract to help prevent diarrhea and it is used in combination with Diphenoxylate an opioid to make you feel better about your diarrhea
Tolterodine
Tolterodine - "I tolt you to hold it until we get there, I'm not stopping for you to use the bathroom again!" Muscarinic Antagonist treats urinary urgency
Oxybutinin
Used to prevent bladder spasm after prostate surgery
Low dose Atropine (0.5 mg)
Dry mouth
&
decreased sweating
Increased dose of Atropine
Tachycardia
Blurred vision
Palpitations
high moderate dose
Decreased GI activity
&
Urinary Retention
High Dose Atropine
CNS effects- stimulation causing restlessness and irritability--> depression --> confusion--> coma - at lower doses it doesn't cross the BBB
Uses for Scopolamine
may cause euphoria, some abuse potential. Used pre-anesthetically to cause sedation, amnesia, and dry bronchial/salivary secretions
Use of antomuscarinic drugs in Parkinson's?
Parkinson's patients have decreased dopamine antimuscarinics will restore the acetylcholine/dopamine balance in the corpus striatum
Cholinergic antagonists in the eye
Block activation of iris sphincter--> mydriasis also causing loss of accommodation to near vision or cycloplegia Tropicamide is a short acting drug used for this in eye examinations. Decreased ciliary muscle tone also decreases aqueous humor drainage especially in narrow angle glaucoma
Antimuscarinic drugs in the heart low dose
low dose = slight bradycardia may occur due to increased ACh release following blockade of presynaptic M2.
Moderate Atropine in the heart
affects postsynaptic M2 receptors at the SA node decreasing vagal tone --> tachycardia. This will also block presynaptic M2 receptors and remove tonic inhibition causing an increase in NE release
Pain can cause a reflex Vagal discharge
Atropine can be used to reveres these effects
Ipratropium
Quat-ammonium (limits effects to lungs) used for bronchodilation in acute asthma attacks and patients with COPD
Solifenacin
Overactive bladder treatment with little effect on salivation
Atropine Poisoning
Dry as a bone
Blind as a bat
Mad as a hatter
Red as a beet
drug classes with anticholinergic effects
Tricyclic antidipressants, antihistamines, antipsychotics
Poisonous mushrooms
some mushrooms contain muscarine and lead to vomiting, diarrhea, vasodilation, tachycardia/bradycardia, sweating, salivation, and possibly bronchoconstriction
Treated with IV atropine