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Pharmacology > Anti-Muscarinic Drugs > Flashcards

Anti-Muscarinic Drugs Flashcards

(56 cards)

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1
Q

Naturally occuring alkaloids

A

Atropine

Scopolamine

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2
Q

Synthetic and Semi-synthetic alkaloids

A

Quaternary ammonium derivatives

Tertiary amine derivatives

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3
Q

Predilection of Atropine

A

Heart
GI
Bronchial smooth muscles

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4
Q

Predilection of Scopolamine

A

Iris sphincter
Ciliary muscle
Exocrine glands

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5
Q

CNS effect of Atropine

A

less BBB permeation (vs scopolamine)

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6
Q

CNS effect of Scopolamine

A

Increased permeation of BBB (vs atropine)

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7
Q

Atropine duration

A

7-14 days

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8
Q

Scopolamine duration

A

3-7 days

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9
Q

Effect of therapeutic dose (0.5-1 mg) of Atropine

A

Almost NO detectable effects (only mild vagal stimulation)

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10
Q

Effect of therapeutic dose (0.5-1 mg) of Scopolamine

A

Prominent central effects
Depression (drowsiness, amnesia, fatigue, dreamless sleep, reduced REM sleep, euphoria)
Occasional excitation (in presence of severe pain)

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11
Q

Which atropine isomeer is more potent?

A

L isomer is 100x more potent

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12
Q

Atropine effects decline rapidly in all organs EXCEPT which organ?

A

Eye (72 hours)

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13
Q

Effect of slow infusion of atropine

A

Paradoxical bradycardia

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14
Q

Drug combination to induce “twilight sleep”

A

Scopolamine + Meperidine (or Demerol)

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15
Q

Quaternary ammonium derivatives used as anti-spasmodic

A 
Glycopyrolate (adjunct for reversal of NM blockade)
Propatheline bromide
Methantheline bromide
Tricyclamol
Anisotropine methylbromide
Clindinium bromide
Hexocyclium methylsulfate
Mepenzolate bromide
Oxyphenonium bromide
Homatropine methylbromide
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16
Q

Quaternary ammonium derivatives used as bronchodilators

A

Ipatropium bromide
Oxytropium bromide
Tiotropium

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17
Q

Tertiary amine derivatives used as mydriatics and cycloplegics

A

Tropicamide
Cyclopentolate
Homatropine hydrobromide

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18
Q

Tertiary amines used as anti-spasmodics (and treatment of acid peptic disease, hypermotility and GU infections)

A 
Dicyclomine hydrochloride / Dicloverine
Tolterodine (on M3 receptor)
Propiverine
Trospium
Oxybutinin chloride
Methixene
Thipenamil
Piperidolate
Oxyphencyclimine hydrochloride
Flavoxate hydrochloride
Tridihexethyl chloride
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19
Q

Anti-spasmodic tertiary amines used for treatment of overactive bladder

A

Tolterodine (on M3 receptor)
Propiverine
Trospium
Oxybutinin chloride

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20
Q

Tertiary amines used as anti-parkinsonism and anti-tremor drugs

A 
Benzotropine mesylate (adjunct)
Trihexyphenidyl (adjunct)
Biperiden (adjunct)
Procyclidin
Diphenhydramine (anti-histamine)
Carmiphen
Orpehadrine citrate
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21
Q

Selective M1 inhibitors

A

Pirenzipine

Telenzipine

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22
Q

Cardiac muscarinic receptor selective

A

Methoctramine

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23
Q

Relative selectivity for glandular and smooth muscles

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A

Hexahydrosiladifenidol

24
Q

Selective M3 receptor blockers

Study These Flashcards
A

Darifenacin
Solifenacin
Fesoteridine

25
Treatment use of selective M3 receptor blockers
Overactive bladder
26
General mechanism of action of antimuscarinics
Reversible COMPETITIVE surmountable blockade; Inhibits binding of Ach Decreased cGMP --> Decreased intracellular calcium
27
Anti-muscarinics are more effective in blocking exogenous or endogenous Ach?
Exogenous
28
Place in decreasing order: Sensitivity of M-receptors to anti-muscarinic agents (atropine is the prototype drug)
1) Salivary, bronchial, sweat glands 2) Smooth muscles of eyes & heart 3) Smooth muscles of GIT & GUT 4) Gastric secretion
29
PK: Absorption
Tertiary amines: well absorbed from GIT & conjunctival membrane (scopolamine absorbed from skin) Quaternary: only 10-30% absorbed from GIT
30
PK: Distribution
Tertiary: widely distributed in tissues/CNS (scopolamine with greatest effect in the CNS) Quaternary: poorly taken up by brain, exists in free form
31
Metabolism & Excretion: Tertiary Amine
Lipid-soluble, penetrate BBB, efficient absorption in post-auricular area, metab in liver, 50% secreted unchanged in urine
32
Metabolism & Excretion: Quaternary
Poorly lipid soluble, Does not cross BBB Better by inhalation, given at the site where it is needed 90% of dose taken orally appears in feces
33
Pharmacologic effects: CNS
Atropine: minimal effects Scopolamine: CNS depressant, prevention of motion sickenss Centrally-acting: Adjunct for Parkinsons (with levadopa), extrapyramidal side effects
34
Pharmacologic effects: Eyes
Mydriasis (not direct effect) Cycloplegia "Sandy eyes" (decreased lacrimation
35
Pharmacologic effects: CVS
``` Modest tachycardia (therapeutic doses) Myocardial depression (very high doses) Little effect on BP Atropine flush (toxic doses) Reduce PR interval ```
36
Pharmacologic effects: Respiratory System
Bronchodilation (d/t blockade of presynaptic receptors) | Reduced bronchial secretions
37
Pharmacologic effects: GIT
Decreased volume of secretions (in large doses)
38
Pharmacologic effects: GUT
Urinary retention
39
Pharmacologic effects: Sweat glands
Xerostomia (mouth) Anhidrosis Causing atropine fever (especially in children)
40
Therapeutic uses: Opthalmologic d/o
Examination of fundus | Anterior uveitis, acute iritis, keratitis, iridocyclitis
41
Therapeutic uses: Respiratory d/o
Hyperactive neural bronchoconstriction reflex (in asthmatics) COPD Bronchial asthma
42
Therapeutic uses: CVS d/o
``` Sinus bradycardia Heart block (d/t digitalis toxicity) Arrythmias in acute MI Angina of MI (parenteral) Hyperactive carotid sinus Idiopathic dilated cardimyopathy ```
43
Therapeutic uses: GIT d/o
NOT a first line treatment Reflux esophagitis Hypermotility and diarrhea
44
Therapeutic uses: CNS disturbance
Parkinson's disease | Motion sickness
45
Therapeutic uses: Anticholinesterase poisoning
Medical emergency Carbamate - Use atropine as antidote Organophosphate - Atropine + pralidoxime **Used for pretreatment
46
Therapeutic uses: Urinary d/o
``` Urolithiasis Enurisis Bladder spasms Urinary incontinence Overactive bladder ```
47
Therapeutic uses: Anesthesia
Adjunct to reverse skeletal muscle relaxation after surgery | Obstetrics
48
Therapeutic uses: Mushroom poisoning
Rapid onset: Parenteral atropine | Late onsent: Atropine NO value
49
Contraindications of anti-muscarinics
Narrow angle glaucoma BPH Obstructive conditions (GUT, GIT atony) Gastric ulcer (do NOT use non-selective)
50
Which contraindication is an ABSOLUTE contraindication
Narrow angle glaucoma
51
Toxicology
``` DRY as a bone BLIND as a bat RED as a beet HOT as a hare MAD as a hatter ```
52
Treatment for anti-muscarinic poisoning
Supportive: artificial respiration hyperthermia control Gastric lavage with activated charcoal (oral) Physostigmine (not SOP) Benzodiazepines (for convulsions)
53
Treatment for anti-muscarinic poisoning d/t quaternary ammonium compunds
ADD neostigmine, sympathomimmetics
54
Drug Interactions: Propantheline + TCA
Additive
55
Drug Interactions: Anti-parkinson
Anti-muscarinic effect ENHANCED
56
Other drug Interactions
Quinidine Phenothiazines Anti-histamines Procainamide

Pharmacology (14 decks)

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