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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
Pilocarpine
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.
26
Pilocarpine ADR
CNS effects, profuse sweating and salivation
27
Major contraindications to use of choline esters
Asthma, hyperthyroidism, coronary insufficiency, and peptic ulcer disease.
28
Ach and agonist antidote
Atropine
29
Ach and agonist route of administration
Oral and subcutaneous for systemic. Sometimes in the eye for local.
30
Undesirable effects of Ach
Flushing, sweating, abd cramping, sensation of tingling in the urinary bladder, difficult visual accommodation, HA, and salivation
31
Indirect-acting Cholinomimetic drugs- Reversible
``` Water soluble Physostigmine Neostigmine Pyrostigmine Edrophonium (tacrine, donepezil, rivastigmine, and galantamine) ```
32
Indirect-acting Cholinomimetic drugs- irreversible/Organophosphates (covalent binding; lipid soluable/cross BBB)
Echothiopate (tx for open angle glaucoma) | Tabun, sarin, soman, parathion, malathion (typically pesticides)
33
Physostigmine
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
Neostigmine, pyridostigmine, edrophonium
Myasthenia gravis, helps w/ reversal of neuromuscular block | Action- amplified effects of Ach, increased muscle strength.
35
Isoflurophate and echothiopate
Glaucoma (not the 1st line therapy | Action- amplifies the effect of Ach
36
Effects of severe acetylcholinesterase inhibition
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
Excessive acetylcholine effects
``` D-Diarrhea U-Urination M-miosis B-bronchoconstriction E-Exitation (CNS or muscle) L-lacrimation S-sweating and salivation ```
38
Nicotinic effects
``` M-Mydriasis, muscle twitching T-tachycardia W- weakness tH- hypertension, hyperglycemia F- fasciculations ```
39
Pralidoxime
Cholinesterase reactivator that breaks bonds between drugs and enzymes if the enzyme has not aged.
40
Effects of muscarinic blocking drugs- CNS
Drowsiness, antimotion sickness action, antiparkinson action, amnesia, delerium
41
Effects of muscarinic blocking drugs- Eye
Clycoplegia, mydriasis, reduction of lacrimal secretion
42
Effects of muscarinic blocking drugs- bronchi
bronchodilation
43
Effects of muscarinic blocking drugs- GI
relaxation, slowed peristalsis
44
Effects of muscarinic blocking drugs-Gu
Relaxation of bladder wall, urinary retention
45
Effects of muscarinic blocking drugs-Heart
Initial bradycardia, then tachycardia
46
Effects of muscarinic blocking drugs-glands
Decreased secretion
47
Antimuscarinic drug- benztropine
Treats manifestation of Parkinson Disease
48
Antimuscarinic drug- scopolamine
prevent or reduce motion sickness
49
Antimuscarinic drug atropine
Produce mydriasis and cycloplegia
50
Antimuscarinic drug- Ipratorium
Bronchodilate in ashtma
51
Antimuscarinic drug- methscopolamine
Reduce transient mobility- used in combination with other antiulcer drugs
52
Antimuscarinic drug- Oxybutinin
Treats transient cystitis and postoperative bladder spasms.
53
Toxicity of antimuscarinic drugs
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
Cause anticholinergic toxicity
Antihistamines-diphenhydramine Tricyclic antidepressants- amitryptyline Atypical antipsychotics- olanzapine Neuroleptic antipsychotics- chlorpromazine
55
Ganglionic Blockers
Interfere w/ postsynaptic transmission | block action of Ach on nicotinic receptors
56
Trimethaphan and Mecamylamine
competitive agonists of Ach at ganglionic nicotinic receptors.
57
Non-depolarizing (competitive)
drugs that bind to nicotinic cholinergic receptors to induce a competitive blockade of Ach (affinity without efficacy) D-tubocurarine
58
Depolarizing (Non-competitive)
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
Long acting duration of action (DOA)
Curare and Pancuronium
60
Intermediate actiong DOA
Cisatracurium and atacurium (metabolism not dependent on hepatic or renal function)
61
Short acting DOA
Mivacurium and succinylcholine
62
Properties of neuromuscular blocking agents- selevtivity
curare is not selective for NMJ
63
Properties of neuromuscular blocking agents- ganglionic block
nicotinic antagonist induces tachycardia and hypotension
64
Properties of neuromuscular blocking agents-Vagolytic
Muscarinic antagonist induces because you are blocking at the ganglia and it stops the end result of muscarninc receptoryou see the muscarinic block.
65
Properties of neuromuscular blocking agents- histimine release
By action on mast cells. Induces bronchospasm, hypotension, airway secretion
66
Botulinum (Botox)
Toxin inhibits Ach release, thus interferes with nerve impulses and causes flaccid paralysis of muscles.

Pharmacotherapeutics I (23 decks)

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