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Pharmacotherapeutics I > Autonomic-Cholinergic Pharmacology > Flashcards

Autonomic-Cholinergic Pharmacology Flashcards

1
Q

Cholinergic recptors

A

Muscarinic and nicotinic

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2
Q

Muscarinic Receptors

A

M1, M2, M3, M4, M5

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3
Q

M1

A

Neural areas- CNS, PNS, gastric parietal cells

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4
Q

M2

A

Cardiac, bladder, lung

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5
Q

M3

A

Glandular- exocrine glands, smooth muscle, bladder, and eye

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6
Q

M1, M3, M5 coupled to G-Proteins

A

Activate second messenger systems responsible for the stimulation of phospholipase C

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7
Q

M2 and M4 coupled to G proteins

A

Responsible for adenyl cyclase inhibition and K+ channel activation

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8
Q

Nicotinic receptors

A

N2 and Nn- autonomic ganglia

N1 or Nm- Neuromuscular junction (NMJ)-somatic motor end plates.

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9
Q

Responses mediated by muscarinic receptors - Heart (AV node and Atria)

A

Decreased heart rate

Decreased AV nodal conduction

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10
Q

Responses mediated by muscarinic receptors - Eyes

A

Contraction of sphincter muscle of iris and ciliary muscles

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11
Q

Response mediated by muscarinic receptors- Gastrointestinal

A

Increased tone, mobility, and secretion

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12
Q

Response mediated by muscarinic receptors- Urinary bladder

A

Relaxation of sphincter

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13
Q

Response of muscarinic receptors- secretory glands (sweat, bronchial, salivary)

A

Increased secretion

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14
Q

Pharmacological properties of choline esters on the Cardiovascular system

A

Vasodilation, decreased cardiac rate, decreased conduction rate, and decreased force of cardiac contraction

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15
Q

Pharmacological properties of choline esters on GI

A

Increase tone, amplitude of contraction, peristaltic activity of stomach and intestines, enhanced secretory activity, and enhanced mobility (accompanied by Nausea, vomiting, belching, intestinal cramping, and defecation)

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16
Q

Pharmacological properties of choline esters on urinary tract

A

Increased ureteral peristalsis, contract of the detrusor muscles of urinary bladder, increased maximal voluntary voiding pressure, and decreased capacity of the bladder.

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17
Q

Bethanechol- cholinergic agonist

A

Acts on receptors M1, M2, M3
Poor substrate for AchE
Sites- smooth musculature of the bladder and GI
Actions- increased intestinal motility and tone, and stimulates detrusor muscles of the bladder while the trigone and sphincter are relaxed causing expulsion of urine.
Therapeutic action- stimulates atonic bladder in postpartum or postoperative urinary renention.

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18
Q

Bethanechol side effects

A

sweating, salivation, flushing, HPOTN, N/D, abd pain and bronchospasm.

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19
Q

Carbachol (carbamylcholine)

A

Poor substrate of AchE with DOA of as long as 1hr
Action- M1, M2, M3 and wak nicotinic agonist-CV and GI systems- may first stimulate then depress, can also cause release of epinephrine for adrenal medulla by its nicotinic acitons.
Therapeutics- used seldomly, sometimes as miotic for gluacoma

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20
Q

Carbachol (Carbamylcholine) adverse reactions

A

Little to no side effects when used in the eye

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21
Q

Methacholine

A

Receptors- M1, M2, M3

Used as diagnostic challenge for bronchial hyperreactivity and asthmatic conditions

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22
Q

Cholinomimetic natural alkaloids and synthetic analogs

A

Pilocarpine, muscarine, and arecoline

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23
Q

Muscarine

A

acts almost exclusively at muscarinic receptor sites

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24
Q

arecoline

A

acts at nicotinic receptor sites

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25
Q

Pilocarpine

A

Dominant muscarinic response at M1, M2, M3
Tertiary amine and less potent
Action- rapid miosis and contraction of the ciliary muscle
Therapeutic use- emergency lowering of the intraocular pressure of both narrow and wide-angle glaucoma.

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26
Q

Pilocarpine ADR

A

CNS effects, profuse sweating and salivation

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27
Q

Major contraindications to use of choline esters

A

Asthma, hyperthyroidism, coronary insufficiency, and peptic ulcer disease.

28
Q

Ach and agonist antidote

A

Atropine

29
Q

Ach and agonist route of administration

A

Oral and subcutaneous for systemic. Sometimes in the eye for local.

30
Q

Undesirable effects of Ach

A

Flushing, sweating, abd cramping, sensation of tingling in the urinary bladder, difficult visual accommodation, HA, and salivation

31
Q

Indirect-acting Cholinomimetic drugs- Reversible

A 
Water soluble
Physostigmine
Neostigmine
Pyrostigmine
Edrophonium (tacrine, donepezil, rivastigmine, and galantamine)
32
Q

Indirect-acting Cholinomimetic drugs- irreversible/Organophosphates (covalent binding; lipid soluable/cross BBB)

A

Echothiopate (tx for open angle glaucoma)

Tabun, sarin, soman, parathion, malathion (typically pesticides)

33
Q

Physostigmine

A

Glaucoma (miosis in the eye); increased intestinal and bladder motility, reverse CNS and cardiac effects of TCA (tricyclic antidepressant); reverse CNS effects of atropine.
Action- amplifies effect of Ach

34
Q

Neostigmine, pyridostigmine, edrophonium

A

Myasthenia gravis, helps w/ reversal of neuromuscular block

Action- amplified effects of Ach, increased muscle strength.

35
Q

Isoflurophate and echothiopate

A

Glaucoma (not the 1st line therapy

Action- amplifies the effect of Ach

36
Q

Effects of severe acetylcholinesterase inhibition

A

Indirect agonists “amplify” action of endogenous acetylcholine.
GI-Diarrhea, urination, salivation
Eye-miosis
Respiratory- bronchoconstriction, increased bronchial secretion
CNS- tremor, anxiety, convulsion, and coma
SKeletal muscle- fasciculation
CV- hypotension

37
Q

Excessive acetylcholine effects

A 
D-Diarrhea
U-Urination
M-miosis
B-bronchoconstriction
E-Exitation (CNS or muscle)
L-lacrimation
S-sweating and salivation
38
Q

Nicotinic effects

A 
M-Mydriasis, muscle twitching
T-tachycardia
W- weakness
tH- hypertension, hyperglycemia
F- fasciculations
39
Q

Pralidoxime

A

Cholinesterase reactivator that breaks bonds between drugs and enzymes if the enzyme has not aged.

40
Q

Effects of muscarinic blocking drugs- CNS

A

Drowsiness, antimotion sickness action, antiparkinson action, amnesia, delerium

41
Q

Effects of muscarinic blocking drugs- Eye

A

Clycoplegia, mydriasis, reduction of lacrimal secretion

42
Q

Effects of muscarinic blocking drugs- bronchi

A

bronchodilation

43
Q

Effects of muscarinic blocking drugs- GI

A

relaxation, slowed peristalsis

44
Q

Effects of muscarinic blocking drugs-Gu

A

Relaxation of bladder wall, urinary retention

45
Q

Effects of muscarinic blocking drugs-Heart

A

Initial bradycardia, then tachycardia

46
Q

Effects of muscarinic blocking drugs-glands

A

Decreased secretion

47
Q

Antimuscarinic drug- benztropine

A

Treats manifestation of Parkinson Disease

48
Q

Antimuscarinic drug- scopolamine

A

prevent or reduce motion sickness

49
Q

Antimuscarinic drug atropine

A

Produce mydriasis and cycloplegia

50
Q

Antimuscarinic drug- Ipratorium

A

Bronchodilate in ashtma

51
Q

Antimuscarinic drug- methscopolamine

A

Reduce transient mobility- used in combination with other antiulcer drugs

52
Q

Antimuscarinic drug- Oxybutinin

A

Treats transient cystitis and postoperative bladder spasms.

53
Q

Toxicity of antimuscarinic drugs

A

Red as a beet, dry as a bone, blind as a bat, mad as a hatter, and hot as a hare
Flushing, dry skin and mucous membranes, mydriasis w/ loss of accommodation, AMS, and fever.

54
Q

Cause anticholinergic toxicity

A

Antihistamines-diphenhydramine
Tricyclic antidepressants- amitryptyline
Atypical antipsychotics- olanzapine
Neuroleptic antipsychotics- chlorpromazine

55
Q

Ganglionic Blockers

A

Interfere w/ postsynaptic transmission

block action of Ach on nicotinic receptors

56
Q

Trimethaphan and Mecamylamine

A

competitive agonists of Ach at ganglionic nicotinic receptors.

57
Q

Non-depolarizing (competitive)

A

drugs that bind to nicotinic cholinergic receptors to induce a competitive blockade of Ach (affinity without efficacy)
D-tubocurarine

58
Q

Depolarizing (Non-competitive)

A

Resistant to AchE so they persist in the synaptic cleft and continually depolarize the neuromuscular end-plate thus the action potential cannot be elicited.
Decamethonium

59
Q

Long acting duration of action (DOA)

A

Curare and Pancuronium

60
Q

Intermediate actiong DOA

A

Cisatracurium and atacurium (metabolism not dependent on hepatic or renal function)

61
Q

Short acting DOA

A

Mivacurium and succinylcholine

62
Q

Properties of neuromuscular blocking agents- selevtivity

A

curare is not selective for NMJ

63
Q

Properties of neuromuscular blocking agents- ganglionic block

A

nicotinic antagonist induces tachycardia and hypotension

64
Q

Properties of neuromuscular blocking agents-Vagolytic

A

Muscarinic antagonist induces because you are blocking at the ganglia and it stops the end result of muscarninc receptoryou see the muscarinic block.

65
Q

Properties of neuromuscular blocking agents- histimine release

A

By action on mast cells. Induces bronchospasm, hypotension, airway secretion

66
Q

Botulinum (Botox)

A

Toxin inhibits Ach release, thus interferes with nerve impulses and causes flaccid paralysis of muscles.

Pharmacotherapeutics I (23 decks)

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