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Botany > CHOLINOCEPTORACTIVATING & CHOLINESTERASEINHIBITING DRUGS > Flashcards

CHOLINOCEPTORACTIVATING & CHOLINESTERASEINHIBITING DRUGS Flashcards

1
Q

 Mimic acetylcholine

A

CHOLINOMIMETIC DRUGS

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2
Q

TYPE OF CHOLINOMIMETIC DRUGS Classified by

A. Spectrum of action (type of receptor activated)

A
  1. Muscarinic

2. Nicotinic

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3
Q

TYPE OF CHOLINOMIMETIC DRUGS Classified by

B. Mechanism of action

A 
1. Direct-acting
 Binding/activate cholinoceptors
2. Indirect-acting
 Inhibiting the hydrolysis of endogenous
ACh
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4
Q

CHOLINOMIMETIC DRUGS

 Divided on the basis of their chemical structure
 Directly bind to and activate muscarinic or
nicotinic receptors
 Many have effects on receptors like ACh

A

A. DIRECT-ACTING CHOLINOMIMETIC DRUGS

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5
Q

BASIC PHARMACOLOGY OF THE DIRECT ACTING CHOLINOCEPTOR STIMULANTS (2)

A
  1. CHOLINE ESTERS
     Including ACh
  2. ALKALOIDS
     Muscarine and nicotine
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6
Q

BASIC PHARMACOLOGY OF THE DIRECT ACTING CHOLINOCEPTOR STIMULANTS
 4 important choline esters
 Permanently charged quaternary NH 4 group
 Relatively insoluble in lipids

A

CHOLINE ESTERS

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7
Q

BASIC PHARMACOLOGY OF THE DIRECT ACTING CHOLINOCEPTOR STIMULANTS
Poorly absorbed
 Poorly distributed in the CNS
 Hydrophilic

A

CHOLINE ESTERS

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8
Q

BASIC PHARMACOLOGY OF THE DIRECT ACTING CHOLINOCEPTOR STIMULANTS
 Hydrolyzed in the GIT
 Differ markedly in their susceptibility to
hydrolysis by cholinesterase

A

CHOLINE ESTERS

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9
Q

BASIC PHARMACOLOGY OF THE DIRECT-ACTING
CHOLINOCEPTOR STIMULANTS

 Very rapidly hydrolyzed
 Large amounts must be infused IV to achieve
concentrations high enough to produce
detectable effects

A

ACETYLCHOLINE

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10
Q

BASIC PHARMACOLOGY OF THE DIRECT-ACTING
CHOLINOCEPTOR STIMULANTS

 Addition of methyl CH3
 3x more resistant to hydrolysis compared to ACh

A

METHACHOLINE

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11
Q

BASIC PHARMACOLOGY OF THE DIRECT-ACTING
CHOLINOCEPTOR STIMULANTS

 Carbamic acid ester derivative of ACh
 More resistant to hydrolysis by cholinesterase
 Longer duration of effect

A

CARBACHOL and BETANECHOL

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12
Q

BASIC PHARMACOLOGY OF THE DIRECT-ACTING
CHOLINOCEPTOR STIMULANTS

 Addition of beta-methyl group (methacholine and
betanechol reduces the potency of these drugs at
nicotinic receptor sites

A

CARBACHOL and BETANECHOL

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13
Q

BASIC PHARMACOLOGY OF THE DIRECT-ACTING
CHOLINOCEPTOR STIMULANT

 Act mostly with muscarinic receptors
(muscarine, pilocarpine)
 Act with nicotinic receptors
(nicotine, lobeline)

A
  1. ALKALOIDS
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14
Q

BASIC PHARMACOLOGY OF THE DIRECT-ACTING
CHOLINOCEPTOR STIMULANT

 Well absorbed from most sites of administration
 Excreted chiefly by the kidneys
 Acidification of urine accelerates clearance of
these amines

A
  1. ALKALOIDS
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15
Q

BASIC PHARMACOLOGY OF THE DIRECT-ACTING
CHOLINOCEPTOR STIMULANT

 Liquid
 Sufficiently lipid-soluble to be absorbed across
the skin

A

NICOTINE

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16
Q

BASIC PHARMACOLOGY OF THE DIRECT-ACTING
CHOLINOCEPTOR STIMULANT

 Quaternary amine
 Less completely absorbed from the GIT
 Toxic when ingested
 Eg, in certain mushrooms, it even enters the brain

A

MUSCARINE

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17
Q

BASIC PHARMACOLOGY OF THE DIRECT-ACTING
CHOLINOCEPTOR STIMULANT

 Plant derivative
 Similar to nicotine

A

LOBELINE

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18
Q

ORGAN SYTEM EFFECTS

 Instilled to the conjunctival sac
 Causes contraction of the sphincter muscle
of iris (miosis)
 Causes ciliary muscle contraction
(accommodation)
A
  1. EYE
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19
Q

ORGAN SYTEM EFFECTS

 Reduction in peripheral resistance and
changes in heart rate

A
  1. CVS
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20
Q

ORGAN SYTEM EFFECTS

 Contraction of the smooth muscles of the
bronchial tree
 Stimulate glands of the tracheobronchial
mucosa to secrete

A
  1. RESPIRATORY SYSTEM
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21
Q

ORGAN SYTEM EFFECTS

 Similar to the parasympathetic nervous
system stimulation
 Increase in the secretory and motor activity
of the gut

A
  1. GIT
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22
Q

ORGAN SYTEM EFFECTS

 Stimulation of the salivary and gastric glands
 Increase in peristaltic activity
 Relaxation of sphincters

A
  1. GIT
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23
Q

ORGAN SYTEM EFFECTS

 Endothelium Derived Relaxing Factor (EDRF)
is released to produce dilation
 Dilation of arteries
 Dilation of veins
 Constriction (high-dose direct effect)
A
  1. BLOOD VESSELS
24
Q

ORGAN SYTEM EFFECTS

 Stimulate the detrussor muscle
 Relax the trigone and sphincter
 Promote voiding

A
  1. GUT
25
Q

ORGAN SYTEM EFFECTS
Stimulate the thermoregulatory sweat,
lacrimal and nasopharyngeal glands

A
  1. GLANDS
26
Q

CHOLINOMIMETIC DRUGS

 Primary effect by inhibiting acetylcholinesterase
which hydrolyzes acetylcholine to choline and
acetic acid

A

B. INDIRECT-ACTING CHOLINOMIMETIC DRUGS

27
Q

CHOLINOMIMETIC DRUGS

 Increase endogenous ACh concentration
 Stimulates cholinoceptors to evoke increase
response

A

B. INDIRECT-ACTING CHOLINOMIMETIC DRUGS

28
Q

CHOLINOMIMETIC DRUGS

 Parasympathetic effects
 Some have direct action at nicotinic receptors

A

B. INDIRECT-ACTING CHOLINOMIMETIC DRUGS

29
Q

CHOLINOMIMETIC DRUGS

 Chief difference of the group are chemical and
pharmacokinetics
 3 chemical groups

A

B. INDIRECT-ACTING CHOLINOMIMETIC DRUGS

30
Q

BASIC PHARMACOLOGY 0F INDIRECT-ACTING
CHOLINOMIMETICS

 Quaternary NH4 group
 2 to10 minutes
 Reversible

A
  1. SIMPLE ALCOHOLS
31
Q

BASIC PHARMACOLOGY 0F INDIRECT-ACTING
CHOLINOMIMETICS

 Quaternary or tertiary NH4 group
 30 minutes to 6 hours
 Reversible

A
  1. CARBAMIC ACID ESTERS OF ALCOHOL
32
Q

BASIC PHARMACOLOGY 0F INDIRECT-ACTING
CHOLINOMIMETICS

 Highly lipid soluble
 Very long duration
 Irreversible

A
  1. ORGANIC DERIVATIVES OF PHOSPHORIC

ACID

33
Q

BASIC PHARMACOLOGY 0F INDIRECT-ACTING
CHOLINOMIMETICS

 Echothiophate
-Retains the very long duration of other
organophosphates
-More stable in aqueous solution

A
  1. ORGANIC DERIVATIVES OF PHOSPHORIC

ACID

34
Q

ORGANIC DERIVATIVES OF PHOSPHORIC
ACID

 Used as insecticides

A

 Parathion and malathion (thiophosphates)

35
Q

 Primary action is to amplify the actions
of endogenous Ach
 Effects are similar, but not always identical,
to the effects of direct-acting cholinomimetics

A

ORGAN SYSTEM EFFECTS

36
Q

ORGAN SYSTEM EFFECTS

 Most prominent effects

A

 CVS
 GIT
 Eye
 Skeletal muscle neuromuscular junction

37
Q

CLINICAL PHARMACOLOGY OF CHOLINOMIMETICS

Pilocarpine
Echothiophate (long-acting effect)
A
  1. EYE
38
Q

CLINICAL PHARMACOLOGY OF CHOLINOMIMETICS

POSTOPERATIVE ILEUS
URINARY RETENTION POST OP

A
  1. GIT and GUT
39
Q
  1. GIT and GUT
    Clinical disorders that involve depression of smooth muscle activity without obstruction
    Betanechol
A

CLINICAL PHARMACOLOGY OF

CHOLINOMIMETICS

40
Q

NEUROMUSCULAR JUNCTION

 Disease affecting the skeletal muscles
neuromuscular junction
 Autoimmune process

A

MYASTHENIA GRAVIS

41
Q 
NEUROMUSCULAR JUNCTION
 
 Production of antibodies that decrease
the functional nicotinic receptors at the
postjunctional end plates
 Cholinesterase inhibitors are used for
therapy
A

MYASTHENIA GRAVIS

42
Q

MYASTHENIA GRAVIS

diagnostic test

A

 Edrophonium

43
Q

MYASTHENIA GRAVIS

long term therapy

A

 Neostigmine, pyridostigmine

44
Q

CLINICAL PHARMACOLOGY OF
CHOLINOMIMETICS

 SUPRAVENTRICULAR TACHYCARDIA
 Treated by short-acting cholinesterase inhibitor
(edrophonium)
 Replaced by newer drugs (calcium channel
blockers)

A
  1. HEART
45
Q
  1. ANTIMUSCARINIC DRUG INTOXICATION

 Lethal in children
 Causes prolonged severe behavioral
disturbances and arrhythmias in adults

A

ATROPINE INTOXICATION

46
Q
  1. ANTIMUSCARINIC DRUG INTOXICATION

 Causes severe muscarinic blockade
 Physostigmine
Antidote to atropine poisoning

A

ATROPINE INTOXICATION

47
Q 
CNS
 ALZHEIMER’S DISEASE
 With anticholinesterase activity
 With cholinomimetic action
 Used for therapy
A

Tacrine

48
Q

TOXICITY

A. DIRECT-ACTING MUSCARINIC STIMULANTS

A 
 Nausea and vomiting
 Diarrhea
 Salivation
 Sweating
 Cutaneous vasodilatation
 Bronchial constriction
 Excitation
 Lacrimation
49
Q

A. DIRECT-ACTING MUSCARINIC STIMULANTS

BLOCKED BY

A

atropine

50
Q

DIRECT-ACTING NICOTINIC STIMULANTS

 40 mg or 1 drop of pure liquid is fatal
2 cigarettes
 Central stimulant action

A

ACUTE TOXICITY

51
Q

DIRECT-ACTING NICOTINIC STIMULANTS

 Convulsion
 Coma
 Respiratory arrest or paralysis
 Hypertension
 Arrhythmia
A

ACUTE TOXICITY

52
Q

DIRECT-ACTING NICOTINIC STIMULANTS

 Treatment is symptom directed
 Atropine
 Anticonvulsants

A

ACUTE TOXICITY

53
Q

DIRECT-ACTING NICOTINIC STIMULANTS

 Smoking

A

CHRONIC TOXICITY

54
Q

RISK OF chronic toxicity increased when

A

Vascular disease
 Peptic ulcers
 60 % carcinogenic

55
Q

C. CHOLINESTERASE INHIBITORS
Major source of intoxication is pesticid
Organophosphates
Treated with large doses of atropine

A

ACUTE TOXICITY

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