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Medications > Autonomic Pharmacology > Flashcards

Autonomic Pharmacology Flashcards

0
Q

Muscarinic ACh Receptors

A

Main antigen is acetylcholine
Parasympathetic post ganglionic neurons
M1, M3, M5: IP3 pathway > increase Ca2+ > SM contraction
M2, M4: inhibit adenyly cyclase and reduce cAMP

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1
Q

Adrenergic Receptors

A

Receptor antigen is norepinephrine or epinephrine (adrenaline: synthesized in adrenal medulla via enzyme phenethanolamine N-methyltransferase)
Sympathetic nervous system

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2
Q

Nicotinic ACh Receptors

A

Preganglionic neurons of parasympathetics, somatic muscle neuromuscular junction
Activation via acetylcholine (release inhibited by botulinum toxin (Botox)

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3
Q

Muscarinic activation

A
  • Slows cardiovascular function
  • Increases secretions
  • increases intestinal activity
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4
Q

Cotinine

A

Main metabolite of nicotine in body

Used for laboratory testing to see if someone smokes

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5
Q

Varenicline

A

partial agonist of a4B2 neuronal nicotinic receptors

Used: treat nicotine dependence and reduces the cravings

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6
Q

Mivacurium

A

nicotinic receptor antagonist (competitive)
Use: neuromuscular blocker = paralyzer
Used in surgeries

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7
Q

Pancuronium

A

nicotinic receptor antagonist (competitive)
Use: neuromuscular blocker = paralyzer
Used in surgeries

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8
Q

Vecuronium

A

nicotinic receptor antagonist (competitive)
Use: neuromuscular blocker = paralyzer
Used in surgeries

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9
Q

Three common organophosphate AchE inhibitors in industry

A

pesticides, parathion, chloropyrifos, malathion (insecticide) and nerve gas (sarin, tabun, VX)
Initial binding to AChE can be reversed but after a few hours, phosphorylated enzyme ages (covalent bond formed) > irreversible

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10
Q

Neostigmine

A

AchE inhibitor
Reversal of non-depolarizing neuromuscular blockers
Use: Treatment of myasthenia gravis
SE: Poisoning > activation of both muscarinic and nicotinic receptors > fatal

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11
Q

Pyridostigmine

A

AchE inhibitor

Use: main treatment for myasthenia gravis

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12
Q

Donepezil (Aricept)

A

AChE Inhibitor

Uses: Palliative treatment of Alzheimer’s disease

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13
Q

Galantamine (Razadyne)

A

AChE Inhibitor

Uses: Palliative treatment of Alzheimer’s disease

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14
Q

Rivastigmine (Exelon)

A

AChE Inhibitor

Uses: Palliative treatment of Alzheimer’s disease

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15
Q

Pralidoxime (2-PAM)

A

Prevents irreversible binding of organophosphate AChE inhibitors to AChE if given prior to a few hours

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16
Q

Toxicity effects of acetylcholinesterase inhibitors

A

DUMBELSS: diarrhea, urination, miosis (contraction of sphincter in eye), bronchoconstrictoin, excitation of muscle (most life threatening) and CNS, lacrimation, salivation, sweating
-Overload of skeletal nicotinin Ach receptors > muscle paralysis > death

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17
Q

Atropine (belladonna)

A

Muscarinic antagonist: tertiary amine that can cross BBB (can cause sedation, behavioral excitation and hallucinations)
Uses: Dilate pupils, treat severe bradycardia
Can be given to help relieve AChE inhibitor poisoning to block muscarinic effects (diarrhea)

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18
Q

Bethanechol

A 
muscarinic agonist (agonist for muscarinic receptors not often used)
Use: treatment of urinary retention
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19
Q

Betanechol, carbachol, pilocarpine

A

Muscarinic agonist
Contract pupillary constrictor > allow aqueous humor to drain out of eye
Uses: Acute glaucoma attack (outflow of aqueous humor into canal of Schlemm is blocked)

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20
Q

SE of anti-muscarinic drugs

A

Decreased secretions (dry mouth), mydriasis (dilated pupil), cycloplegia (decreased accommodation), hyperthermia, tachycardia, sedation (BBB), bronchodilation, urinary retention, constipatoin, behavior excitation and hallucinations (BBB)

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21
Q

Scopolamine

A 
Muscarinic antagonist (can cross BBB)
Use: motion sickness due to sedative and amnesiac effects
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22
Q

Glycopyrrolate

A

Muscarinic antagonist

Use: Dry secretions to prevent aspirations of fluids

23
Q

Benztropine

A

Muscarinic antagonist

Use: Parkinsonism (including drug induced)

24
Q

Tropicamide

A

Muscarinic antagonist

Use: dilate pupils (shorter acting than atropine), more effective in clinical ophthalmology visit

25
Q

Ipratropium

A

Muscarinic antagonist
Use: treat asthma and COPD
Combined with albuterol (B-agonist) as an inhaler

26
Q

Tolerodine

A

Muscarinic antagonist

Use: treat bladder spasm and urinary incontinenct

27
Q

Solifenacin

A

Muscarinic antagonist

Use: treat bladder spasm and urinary incontinenct

28
Q

Tiotropium (Spiriva)

A

Muscarinic antagonist
Use: treat COPD
Capsuled form that is pierced > aerosolized and inhaled

29
Q

Treatment of urinary incontinence and overactive bladder

A

Tolterodine, oxybuynin, solifenacin

Muscarinic antagonists

30
Q

Amitriptyline (Elavil)

A

Tricylic antidepressant with antimuscarinic properties

Overdose > fatal due to antimuscarinic effects (cardiac arythmias)

31
Q

How do you treat anti-muscarinic overdose

A

AChE inhibitors

32
Q

How do you treat AChE overdose

A

Atropine

33
Q

alpa Adrenergic receptors

A

a1: increase IP3, diacylglycerol and intraellular Ca+ > SM contraction (determinant of systemic BP)
a2: inhibit adenylyl cyclase > decreased calcium influx > decreased release of norepinephrine (located at presynaptic terminals > inhibit neurotransmitter release > reduce central adrenergic effects)

34
Q

Beta adrenergic receptors

A

All activate adenylyl cyclase + increase intracellular cAMP
B1: expressed in heart > increase HR
B2:dilate/relax SM>vasodilation, bronchodilation and uterine relaxtation
B3: lipolysis of adipose tissue + relaxation of urinary bladder

35
Q

alpha1-adrenergic receptor activation

A

mydriasis (pupil dilation), vasoconstriction, contraction of bladder trigone + sphincter (urinary retention), SM contraction of prostate

36
Q

Phenylephrine

A

alpha1-adrenergic receptor agonist

Use: treat nasal congestion (constrict vessels), IV > raise BP in acute setting

37
Q

Clonidine

A

alpha2-agonist
UsE: treat hypertension > reduce central norepinephrine release
SE: rebound hypertension if stopped abruptly

38
Q

Prazosin

A

alpha1-adrenergic receptor antagonist (specific)

Use: treatment of hypertension via vasodilation

39
Q

Terazosin

A

alpha1-adrenergic receptor antagonist (specific)

Use: treatment of benign prostatic hypertrophy > relaxes prostate capsular SM

40
Q

Phenoxybenzamine

A

Non-specific (a1+a2) alpha-adrenergic antagonist

Use: manage pheochromocytoma (tumor that secretes catecholamines)

41
Q

Phentolamine

A

Non-specific (a1+a2) alpha-adrenergic antagonist

Use: manage pheochromocytoma (tumor that secretes catecholamines)

42
Q

B1-adrenergic receptor activation

A

Increased heart rate (SA node), increased conduction velocity (AV node), increased force of contraction (atrial + ventricular muscle)

43
Q

Dobutamine

A

B-1 adrenergic receptor agonist

Use: treat cardiogenic shock and heart failure

44
Q

B-blockers (B-1adrenergic receptor antagonist) action

A

Treat angina, hypertension, arrhythmias

45
Q

B2-adrenergic receptor effects

A

vasodilation (all vessels), decreased pre-load, muscle tremor, glycogenolysis, uterine relaxation, bronchodilation

46
Q

Albuterol

A

B2-adrenergic receptor agonist
Use: shorta acting inhaler for acute asthma attacks
SE: also activates B1 > tachycardia

47
Q

Salmeterol

A

B2-adrenergic receptor agonist (selective)
Use: long acting (not used for asthma attacks) for chronic asthma
SE: increased risk of asthma death

48
Q

Formoterol

A

B2-adrenergic receptor agonist (selective)
Use: long acting (not used for asthma attacks) for chronic asthma
SE: increased risk of asthma death

49
Q

Bambuterol

A

B2-adrenergic receptor agonist (selective)
Use: long acting (not used for asthma attacks) for chronic asthma
SE: increased risk of asthma death

50
Q

Terbutaline

A

B2- adrenergic receptor agonist

Use: no longer (black box) fast-acting bronchodilator and also use in uterine relaxation to stop premature labor

51
Q

Isoproterenol

A

non-selective B-adrenergic agonist
Use: treatment of bradycardia (effects blocked by B-blockers)
Mechanism: B2 effect = lower vascular resistance B1 effect = increase HR and contractility

52
Q

Mirabegron

A

B3-adrenergic receptor agonist
Use: treatment of overactive bladder
Relax urinary bladder SM + enhance lipolysis

53
Q

Norepinephrine

A

a+B adrenergic receptor agonist (B1 more than B2)
Use: Increase BP
Effects: Increase SBP, DBP > vagal response > slow HR, increase peripheral vascular resistance

54
Q

Epinephrine

A

a+B-adrenergic receptor agonist
Use: cardiac arrest, anaphylaxis, severe asthma (results in increase SBP, decrease DBP = increase MAP, accelerated HR)
Effects: vasoconstriction of vascular beds (precapillary vessels, a1), increase HR (B1), increase contraction (B1), bronchodilation (B2), vasodilation of large vessels in skeletal muscle (B2)

Medications (3 decks)

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