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Pharmacology > Anti-Muscarinic Drugs > Flashcards

Anti-Muscarinic Drugs Flashcards

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

A

Hexahydrosiladifenidol

24
Q

Selective M3 receptor blockers

A

Darifenacin
Solifenacin
Fesoteridine

25
Q

Treatment use of selective M3 receptor blockers

A

Overactive bladder

26
Q

General mechanism of action of antimuscarinics

A

Reversible COMPETITIVE surmountable blockade; Inhibits binding of Ach
Decreased cGMP –> Decreased intracellular calcium

27
Q

Anti-muscarinics are more effective in blocking exogenous or endogenous Ach?

A

Exogenous

28
Q

Place in decreasing order: Sensitivity of M-receptors to anti-muscarinic agents (atropine is the prototype drug)

A

1) Salivary, bronchial, sweat glands
2) Smooth muscles of eyes & heart
3) Smooth muscles of GIT & GUT
4) Gastric secretion

29
Q

PK: Absorption

A

Tertiary amines: well absorbed from GIT & conjunctival membrane (scopolamine absorbed from skin)
Quaternary: only 10-30% absorbed from GIT

30
Q

PK: Distribution

A

Tertiary: widely distributed in tissues/CNS (scopolamine with greatest effect in the CNS)
Quaternary: poorly taken up by brain, exists in free form

31
Q

Metabolism & Excretion: Tertiary Amine

A

Lipid-soluble, penetrate BBB, efficient absorption in post-auricular area, metab in liver, 50% secreted unchanged in urine

32
Q

Metabolism & Excretion: Quaternary

A

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
Q

Pharmacologic effects: CNS

A

Atropine: minimal effects
Scopolamine: CNS depressant, prevention of motion sickenss
Centrally-acting: Adjunct for Parkinsons (with levadopa), extrapyramidal side effects

34
Q

Pharmacologic effects: Eyes

A

Mydriasis (not direct effect)
Cycloplegia
“Sandy eyes” (decreased lacrimation

35
Q

Pharmacologic effects: CVS

A 
Modest tachycardia (therapeutic doses)
Myocardial depression (very high doses)
Little effect on BP
Atropine flush (toxic doses)
Reduce PR interval
36
Q

Pharmacologic effects: Respiratory System

A

Bronchodilation (d/t blockade of presynaptic receptors)

Reduced bronchial secretions

37
Q

Pharmacologic effects: GIT

A

Decreased volume of secretions (in large doses)

38
Q

Pharmacologic effects: GUT

A

Urinary retention

39
Q

Pharmacologic effects: Sweat glands

A

Xerostomia (mouth)
Anhidrosis
Causing atropine fever (especially in children)

40
Q

Therapeutic uses: Opthalmologic d/o

A

Examination of fundus

Anterior uveitis, acute iritis, keratitis, iridocyclitis

41
Q

Therapeutic uses: Respiratory d/o

A

Hyperactive neural bronchoconstriction reflex (in asthmatics)
COPD
Bronchial asthma

42
Q

Therapeutic uses: CVS d/o

A 
Sinus bradycardia
Heart block (d/t digitalis toxicity)
Arrythmias in acute MI
Angina of MI (parenteral)
Hyperactive carotid sinus
Idiopathic dilated cardimyopathy
43
Q

Therapeutic uses: GIT d/o

A

NOT a first line treatment
Reflux esophagitis
Hypermotility and diarrhea

44
Q

Therapeutic uses: CNS disturbance

A

Parkinson’s disease

Motion sickness

45
Q

Therapeutic uses: Anticholinesterase poisoning

A

Medical emergency
Carbamate - Use atropine as antidote
Organophosphate - Atropine + pralidoxime
**Used for pretreatment

46
Q

Therapeutic uses: Urinary d/o

A 
Urolithiasis
Enurisis
Bladder spasms
Urinary incontinence
Overactive bladder
47
Q

Therapeutic uses: Anesthesia

A

Adjunct to reverse skeletal muscle relaxation after surgery

Obstetrics

48
Q

Therapeutic uses: Mushroom poisoning

A

Rapid onset: Parenteral atropine

Late onsent: Atropine NO value

49
Q

Contraindications of anti-muscarinics

A

Narrow angle glaucoma
BPH
Obstructive conditions (GUT, GIT atony)
Gastric ulcer (do NOT use non-selective)

50
Q

Which contraindication is an ABSOLUTE contraindication

A

Narrow angle glaucoma

51
Q

Toxicology

A 
DRY as a bone
BLIND as a bat
RED as a beet
HOT as a hare
MAD as a hatter
52
Q

Treatment for anti-muscarinic poisoning

A

Supportive: artificial respiration hyperthermia control
Gastric lavage with activated charcoal (oral)
Physostigmine (not SOP)
Benzodiazepines (for convulsions)

53
Q

Treatment for anti-muscarinic poisoning d/t quaternary ammonium compunds

A

ADD neostigmine, sympathomimmetics

54
Q

Drug Interactions: Propantheline + TCA

A

Additive

55
Q

Drug Interactions: Anti-parkinson

A

Anti-muscarinic effect ENHANCED

56
Q

Other drug Interactions

A

Quinidine
Phenothiazines
Anti-histamines
Procainamide

Pharmacology (14 decks)

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