Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

MOHDIII - Unit 2 > Autonomic Pharmacology > Flashcards

Autonomic Pharmacology Flashcards

1
Q

Muscarinic receptor agonists

A
  • bethanechol
  • carbachol
  • pilocarpine
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Muscarinic receptor antagonists

A

atropine, glycopyrrolate, ipratropium, scopolamine, solifenacin, tolterodine, tropicamide

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Sympathetic nervous system (SNS)

A
  • increased heart rate, pupillary dilation, reduced GI perstalsis
  • neurotransmitter: NE, receptor: adrenergic
  • exception: some sweat glands use muscarinic acetylcholine receptor
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Parasympathetic nervous system (PNS)

A
  • increased salivation, increased peristalsis, decreased heart rate
  • neurotransmitter: acetylcholine (ACh), receptor: muscarinic
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Catecholamine (dopamine, NE, epinephrine) synthesis

A
  • rate limiting step: tyrosine>L-DOPA (tyrosine hydroxylase)
  • epinephrine synthesized in adrenal medulla (PHENETHANOLAMINE-N-METHYLTRANSFERASE) from norepinephrine
  • dopamine effects are in renal smooth muscle
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Acetylcholine (Cholinergic) receptors

A
  • muscarinic (certain mushrooms) & nicotinic (tobacco plant)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Muscarinic receptors

A 
M1: neural
M2: cardiac
M3: glandular/smooth muscle
M4: CNS
M5: unclear role in vivo
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Odd-numbered (M1,M3,M5) muscarinic receptors

A
  • act via inositol triphosphase (IP3) involved in smooth muscle contract
  • vasodilation, bronchoconstriction, increased GI motility, increased salivation, increased sweating, voiding, defacation
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Even numbered (M2,M4) muscarinic receptors

A
  • inhibit adenylyl cyclase & reduce cyclic AMP (cAMP)

- M2: opening of K+ channels & inhibition of Ca2+ channels slowing heart rate and decreasing contractility

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Nicotinic acetylcholine receptors

A
  • muscle & neuronal types
  • muscle: skeletal muscle, mediates contraction
  • neuronal: both PNS & SNS
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Nicotinic acetylcholine receptor agonists

A
  • prominent actions on neuronal receptors both in brain and autonomic ganglia
  • minimal actions on muscle type receptors
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Nicotine pharmacology

A
  • CNS activation of receptors in regions involved w/ cognitive functions and reward
  • autonomic effects: tachycardia, increased atrial pressure, sweating
  • metabolite is cotinine: lab testing can tell smokers from non smokers from nicotine replacement
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Varenicline

A
  • partial agonist at the alpha4beta2 subtype of neuronal nicotinic receptor
  • mediates reward effect of nicotine
  • shown to help treat nicotine dependence
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Nicotinic acetylcholine receptor antagonists

A
  • antagonists of muscle type receptors used as neuromuscular blocker
  • mivacurium, pancuronium, vecuronium
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Acetylcholinesterase inhibitors

A
  • increase amount of ACh in synaptic cleft at both nicotinic and muscarinic synapses
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Clinical uses of AChe inhibitors

A
  • neuromuscular reversal agents
  • myasthenia gravis
  • alzheimer’s disease
  • insecticides
  • nerve gases
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Myasthenia gravis

A
  • caused by antibodies targeted against muscle type nicotinic acetylcholine receptor resulting in fatigue/muscle weakness
  • treatment: long acting AChE inhibitor pyridostihmine
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Alzheimer’s disease

A
  • AChE inhibitors that penetrate CNS
  • donepezil, rivastigmine, galantamine
  • limited effect often with only improvement for less than a year
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Toxicologic importance of AChE inhibitors

A
  • insecticides: chlorpyrifos, parathion, malathion
  • nerve gases: VX, sarin, tabun
  • organophasphate insecticide AChE inhibitors can cause irreversible inhibition of AChE after several hours of exposure
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

AChE inhibitor poisoning

A
  • Diarrhea, Urination, Miosis, Bronchoconstriction (PNS), Excitation (muscle & CNS), Lacrimation, Salivation, Sweating
  • DUMBELSS
  • treatment: respiratory support most important-ATROPINE, if organophasphate AChE poisoning-PRALIDOXIME
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Muscarinic acetylcholine receptor agonists

A
  • used to treat glaucoma, urinary retention, dry mouth (xerostomia)
  • bethanechol, carbachol, pilocarpine used topically for glaucoma
  • bethanechol used to manage urinary retention
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Muscarinic acetylcholine receptor antagonists

A
  • ATROPINE, tricyclic antidepressants (amitriptyline & diphenhydramine)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Effects of anti-muscarinic drugs

A
  • decreased secretions (dry mouth), mydriasis (dilated pupils), cycloplegia (decreased accommodation), hyperthermia, tachycardia, bronchodilation, urinary retention & constipation
  • sedation, behavioral excitation & hallucinations seen with drugs that cross blood brain barrier
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Clinical applications of antimuscarinics

A
  • sever bradycardia: atropine
  • acetylcholinesterase poisoning: atropine
  • pupil dilation for ophthalmology: tropicamide
  • motion sickness: scopolamine
  • dry secretions: glycopyroolate
  • parkinsonism: benztropine & diphenhydramine
  • asthma & COPD: ipratropium, tiotropium
  • bladder spasm, urinary incontinence: tolterodine, solifenacin
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

Toxicity of antimuscarinic agents

A
  • hyperthermia, tachycardia, cardiac arrhythmias, sedation, behavioral excitation, hallucinations
  • AChE inhibitors used in management
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

Adrenergic receptors

A
  • alpha1, alpha2, beta1, beta2, beta3
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

Alpha 1 adrenergic receptor

A
  • increase inositol triphosphate (IP3), diacylglycerol, intracellular Ca2+
  • contract smooth muscle leading to vasoconstriction
  • urinary retention, dilates pupils
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

Alpha 2 adrenergic receptors

A
  • inhibit adenylyl cyclase
  • constrict vascular smooth muscle
  • presynaptic receptors in CNS that inhibit NE release
29
Q

Beta adrenergic receptors common effect

A
  • activate adenylyl cyclase & increase intracellular cAMP
30
Q

Beta 1 adrenergic receptor

A
  • predominately in the heart

- increased heart rate & contractility

31
Q

Beta 2 adrenergic receptor

A
  • dilate or relax smooth muscle, causing vasodilation, bronchodilation, and uterine relaxation
32
Q

Beta 3 adrenergic receptor

A
  • lipolysis of adipose tissue & relaxation of urinary bladder
33
Q

Alpha 1 adrenergic agonists

A
  • mydriasis (dilated pupils), vasoconstriction, urinary retention, contraction of smooth muscle of prostate gland
  • specific alpha 1 agonist is PHENYLEPHRINE: used to treat nasal congestion by limiting blood flow to nasal mucosa, & when given through IV in hospital to raise blood pressure
34
Q

Alpha 2 adrenergic agonists

A
  • CLONIDINE is specific alpha 2 agonist that activates presynaptic receptor that has an inhibitory effect on SNS
  • clonidine prone to cause REBOUND HYPERTENSION if drug is stopped abruptly
35
Q

Alpha 1 specific antagonists

A
  • prazosin, doxazosin, terazosin, tamsulosin
  • prazosin & doxazosin used to treat HTN
  • terazosin & tamsulosin used to treat BPH
  • all can cause orthostatic hypotension especailly prazosin
36
Q

Alpha 2 specific antagonists

A
  • yohimbine

- not used clinically but is purported to have aphrodisiac effects

37
Q

Non-specific antagonists of alpha adrenergic receptors

A
  • phenoxybenzamine (IRREVERSIBLE) & phentolamine

- management of PHENOCHROMOCYTOMA to block catecholamines released by these tumors

38
Q

Acetylcholinesterase inhibitors

A
  • donepezil
  • insecticides
  • neostigmine
  • pyridostigmine
  • rivastigminea
39
Q

Beta 1 adrenergic agonists

A
  • dobutamine: used to treat cardiogenic shock and heart failure
40
Q

Beta 2 adrenergic agonists

A
  • used to treat asthma and rarely to stop premature labor
41
Q

Albuterol

A
  • short acting B2 agonist used for asthma attacks

- also activates B1 receptors and can cause tachycardia

42
Q

Salmeterol, formoterol, bambuterol

A
  • LONG ACTING selective B2 agonists used for chronic asthma therapy
  • association of these drugs w/ increased risk of asthma death
43
Q

Terbutaline

A
  • B2 agonist that can be used to halt premature labor
  • B2 agonists cause relaxation of uterine smooth muscle
  • safety concerns so terbutaline is now discouraged
44
Q

Isoproterenol

A
  • NON SELECTIVE Beta adrenergic agonist that lowers PVR (B2) and increases heart rate & contractility (B1)
  • used primarily for symptomatic bradycardia
  • effects blocked by non selective B-blocker like propranolol/nadolol
45
Q

Beta 3 adrenergic agonists

A
  • MIRABEGRON: used to treat overactive bladder
46
Q

Agonists of both alpha and beta receptors

A
  • norepinephrine

- epinephrine

47
Q

Norepinephrine

A
  • potent a1,a2, & B1 but little action at B2
  • used in septic shock to increase BP through increased PVR & HR
  • systolic and diastolic pressure increase, which triggers compensatory vagal action to slow heart rate, PVR increases while cardiac output is unchanged or decreased
48
Q

Epinephrine

A
  • potent agonist at both alpha and beta receptors
  • dilate bronchial smooth muscle & raise blood pressure
  • management of anaphylactic shock
49
Q

Epinephrine blood pressure effects

A
  • modest rise in arterial pressure
  • increase in systolic pressure and a decrease in diastolic pressure
  • pulse rate increases
50
Q

Epinephrine combined with alpha adrenergic antagonist

A
  • B agonist effect are now unopposed
  • increased heart rate (B1) & vasodilation (B2) & drop in MAP
  • this is called EPINEPHRINE REVERSAL
51
Q

Beta antagonist (B blockers) clinical uses

A

hypertension, cardiac arrhythmias, heart failure, angina, anxiety, muscle tremors, hyperthyroidism, glaucoma

52
Q

Non selective beta blocker

A
  • propranolol: used to treat anxiety, muscle tremors, hyperthyroidism because B2 receptors are involved in these disorders
53
Q

Glaucoma treatment

A
  • timolol: topically used to reduce aqueous humor secretion
54
Q

Adverse effects of B-blockers

A
  • bradycardia, AV conduction block, hypotension, sexual dysfunction
  • *non-selective B-blockers should be avoided in asthma patients due to bronchoconstriction caused by B2 receptors. non selective agents can also cause problems in diabetic patients blocking glycogenolysis (B2 effect)
55
Q

Selectivity of B-blockers

A
  • selective B1: atenolol, metoprolol, esmolol
56
Q

Carvedilol & labetalol

A
  • block a1, B1, & B2
  • carvedilol: manage heart failure
  • labetalol: hypertension in pregnancy
57
Q

Esmolol

A
  • selective B1 blocker
  • IV administration w/ short duration of action (minutes)
  • acute management of cardiac arrhythmias
58
Q

Nadolol duration of action

A
  • long acting

- half life of ~24 hours

59
Q

Acebutolol & pindolol

A
  • B blockers w/ partial agonist effect
  • INTRINSIC SYMPATHOMIMETIC ACTIVITY
  • act as antagonist when there is high adrenergic activity
  • theoretic advantage is that they should cause less bradycardia
60
Q

Amphetamine effects

A
  • increase norepinephrine release from nerve terminals
  • increase release of dopamine (schizophrenic like symptoms)
  • NO ANTIDOTE
61
Q

Amphetamine & amphetamine like drugs (related to ephedrine and pseudoephedrine)

A
  • amphetamine (adderall)
  • methamphetamine
  • MDMA/ecstasy
  • MDA
  • bath salts
62
Q

Amphetamine clinical uses

A
  • ADHD
  • amphetamine mixed salts (adderall)
  • lisdexamfetamine (vyvanse): prodrug, lysine linked to dextroamphetamine
  • short term weight loss & narcolepsy
63
Q

Methamphetamine

A
  • abused drug is d-methamphetamine
  • levo (l-) isomer marked as Vicks vapor inhaler
  • only one prescription form on market (desoxyn): limited use for obesity and ADHD
  • smoking or injecting meth associated w/ binge use
64
Q

Bath salts

A
  • misleading name for illicit amphetamine like drugs
  • related to cathinone and amphetamines: mephedrone, MDPV, methylone
  • causes hallucinations and panic attacks
65
Q

Cocaine

A
  • blocks norepinephrine & dopamine reuptake
  • schedule II drug w/ limited use as local anesthetic in ENT surgeris
  • NO ANTIDOTE
66
Q

Cocaine metabolism

A
  • half life varies from 30 min (chronic users) to 11 hrs (newborn)
  • diagnostic metabolite is BENZOYLECGONINE (drug test target)
  • traces remain in body for weeks
67
Q

Health complications of cocaine

A
  • myocardial infarct, strokes, brain hemorrhage, seizures, birth defects, placental abruption (constricts placental vessels)
  • increased risk of birth defects, stimulates uterine contractions
  • crack cocaine: crack mixed with bicarbonate
68
Q

Cocaine facts

A
  • fatal cocaine use: death not related to blood levels, large hearts found with chronic users
  • perforated septum is common, burns on hands, lips, injection sites
  • dopamine effects: euphoria & paranoia

MOHDIII - Unit 2 (23 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions