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pda 1 > adrenergics > Flashcards

adrenergics Flashcards

1
Q

catecholamines and sympathomimetics

A

peripheral excitatory action on smooth muscle (blood vessel, radial muscle, glands)
peripheral inhibitory action on smooth muscle (gut, bronchial tree, blood vessels in muscle)
cardiac excitatory action that increases heart rate and contraction
metabolic actions (increases glycogenolysis, lipolysis)
endocrine actions: decrease insulin release, increase renin release
CNS: resp stim, increase wakefulness, psychomotor activity, reduction in appetite

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2
Q

endogenous catecholamines

A

norepinephrine, epinephrine, and dopamine

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3
Q

epinephrine

receptor selectivity, CV effects, Resp effects, metabolic effects, absorption/fate and excretion, therapeutic uses

A

naturally occuring, synthesized in adrenal medulla

Receptor selectivity: a1 a2 B1 B2
Cv effect: potent vasopressor via (a1) can dialate some beds at low loses (B2), with large bolus- rapid increase in BP (a1) and increase in HR/cont/CO (B1). w/ low dose- increase in HR/cont/CO B1, increase in systolic pressure, but decrease in diastolic pressure (B2 dialation of sk muscle) MAP doesnt change

Resp: powerful bronchodilation (B2)

met: increase in glucose and fatty acids in blood
abftex: not effective with oral, short T12

Therapeutic uses: releif of hypersensitivity reaction to drugs and other allergens, co administered with anesthetics to increase duration, bradyarrhthmias
ophthalmic uses: mydriatic, decrease hemorrhage, conjuctival decongestion

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4
Q

Norepinephrine

receptor selectivity, CV effects, Resp effects, metabolic effects, absorption/fate and excretion, therapeutic uses

A

receptor selectivity (a1 a2 B1)

CV: a1 mainly, PVR up, increases BP, can cause reflex bradycardia

resp: no B 2 activity
abftex: like epi
therapeutics: used as a vasoconstrictor shock hypotension

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5
Q

dopamine

receptor selectivity, CV effects, therapeutic uses

A

receptor selectivity (D1, B1 a1

CV: low doese (D1 receptro effects), vasodilation of renal and mesenteric aa, decrease peripheral receptors

med dose (D1 and B1) increase HR/cont/CO increases systolic w/o diastolic

high dose (D1 B1 a1 effects)- cardiostimulation and genrealized vasoconstriction

therapeutic uses: sever decompensated hrt failure shock, only used IV

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6
Q

non selective B-adrenergic receptor agonists

A

isoproterenol, dobutamine,

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7
Q

Isoproterenol receptor selectivity, CV effects, Resp effects, metabolic effects, absorption/fate and excretion, therapeutic uses

A

receptors: B1 and B2
CV: decrease PR, increased HR/Cf/CO, decreased MAP
resp: bronchodilation
abftex: metabolized by COMT in liver, duration of action is brief

therapeutic: emergency use (IV) to stimulate HR during bradycardia/heart block

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8
Q

dobutamine receptor selectivity, CV effects, Resp effects, metabolic effects, absorption/fate and excretion, therapeutic uses

A

receptor selectivity: (-) and (+) isomers
- isomer: a1 agonist and B agonist
+ isomer: a1 antagonist and B agonist
racemic mix for overall B1 agonist effects

CV effects: increased CR/cont/CO
minimal change in peripheral resist and BP

therapeutics: short T.5 admin IV, short term of cardiac decompensation
cardiac stress test

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9
Q

B2- selective adrenergic agonists

A

Albuterol (short acting) and Salmeterol (long)

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10
Q

albuterol receptor

A

act on B2 adrenergic receptors, adrenergic receptors, administered by inhalation or orally

short acting relief of bronchoconstriction

side effects: tremor anxiety and tachycardia (B1 activation)

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11
Q

salmeterol

A

B2 receptor only inhaled, long acting, with inhalation

COPD, moderate or severe persistent asthma, not suitable for monotherapy

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12
Q

a1- selective adrenergic receptor agonist

A

phenylephrine

potent vasoconstrictors due to stimulation of alpha1 receptors in vascular smooth muscle

clinical utility of the drugs is limited but treat for hypotension

some useful as nasal decongestant

acts only on alpha1 (increases systolic and diastolic BP, decreases HR (reflex), decreases blood flow to most vascular receptors

therapeutics:
ophthalmic: mydriatic
nasal decongestant
hypotension

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13
Q

a2 selective adrenergic receptor agonists

A

clonidine, methyldopa

used for the treatment of systemic hypertension
lower BP via CNS represses sympathetic tone

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14
Q

clonidine

A

orally active a2 agonist reduces sympathetic outflow

decreases peripheral resistance HR and CO

Major therapeutic use: anti hypertensive agent
side effects: occur in 50% of pts (drymouth and sedation)

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15
Q

methyldopa

A

orally active prodrug
methyldopamine-> methyl NE
treats hypertension in pregnancy

sedation and dry mouth

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16
Q

tyramine

A

indirect acting sympathomimetic
releases NE from sympathetic nerves cause sympathomimetic actions
not used as a therapeutic, found in high levels in certain foods (wines beer cheese) MAO-A inactivates it

in patients taking MAO inhibitors, ingestion of tyramine can cause hypertensive crisis

17
Q

amphetamine

A

powerful CNS stimulation and sympathomimetic actions

effective after oral administration- long t1/2

d more effective than I

releases NE and other biogenic amines dopamine from storage sites in nerve terminals

CNS- stimulant, appetite suppresant, stimulates resp

dependance and tolerance can develop
for narcolepsy and ADHD

18
Q

pseudophedrine

A

direct a1 agonist activity with slight B2 agonist activity (orally effective but less CNS stim than amphetamine

major therapeutic use nasal decongestant (a1)

19
Q

adrenergic neuron blocker

A

drugs that disrupt adrenergic neuron function by inhibiting the synthesis, storage, release of NE

drugs historically used as antihypertensive agents

Guanethidine and guanadrel, reserpine

20
Q

guanethidine and guanadrel

A

inhibit NE release and deplete neuronal stores

orally active compounds used to treat severe hypertenstion

Guanethidine, polar compound, does not enter CNS
long acting, taken into adrenergic nerves by the NE transporter (NET)- effects inhibited by tricyclic anti depressents, side effects lots including orthostatic hypotension sexual function, diarrhea, muscle weakness, edema

21
Q

reserpine

A

diffuses into adrenergic nerves, transport doesnt require the NET

treats hypertension, can enter brain and CNS (dpression suicide) sedation

22
Q

adrenergic receptor antagonists

A

inhibit the interaction of NE, epi, and sympathomimetics

compounds have been devlpd that have different binding affinities fot the various receptors

23
Q

alpha blockers

A

specifically block a receptors

a1: arterial/venous visceral smooth muscle (prostate and bladder)
a2: inhibition of NE from nerve terminals

24
Q

non selective a blockers

A

phenoxybenzamine, phentolamine both block both a1 and a2

phenoxybenzamine- irreversible antagonist- orally active long duration, block lasts, need to resynthesize receptors

phentolamine- competitive reversible antagonist, orally active block can be overcome by agonist

use for pheochromocytoma

sid e: hypotension reflex cardiostimulation (tachycardia)

25
Q

a1- specific blockers

A

prazosin and tamsulosin

26
Q

Prazosin

A

orally active competitve blocker, minimal tachycardia bc of a1 only

decreases vascular tone
produces favorable effects on lipid profile

hyper tension and shrt term treatment of congestive heart failure

1st dose orthostatic hypotension

27
Q

tamsulosin

A

favors prostate

effective for treatment of benign prostatic hyperplasia

no hypertension

28
Q

B blockers

A

3 classes: non subtype selective (first gen), B1 selective (2nd gen), B antagonist w/ additional CV actions

29
Q

general B blocker effects of CV effects, Resp effects, metabolic effects, absorption/fate and excretion, therapeutic uses

A

CV: slows HR/cont, reduces sinus rate, lowers BP
Pulm: B2 blockade can cause bronchoconstriction

metab: lowers glucose and lipid in blood vessels
pertension)
side effects: cv (heart failure), brady cardia; pulm exacerbate COPD and asthma; CNS fatigue, sleep disturbances; met (hypoglycemia);

use to treat CV disease (angina hy), glaucoma, tremors

30
Q

non specific B blocker

A

propranolol, Timolol

31
Q

propranolol

A

orally bioavailable large 1st passs w/ shot T12 enters CNS

hypertension, angina, cardiac arrythmia, MI, pheochromcytoma, tremmors

32
Q

timolol

A

no intrinsic activity

33
Q

B1 selective blockers

A

both have decreased pulm side effects

metoprolol, atenolol (less CNS)

34
Q

third generation B blockers

A

have other CV actions
Labetalol: antagonist of a1 B1 B2 (emergency hypertension)

Carvedilol: anagonist of a1 B1 B2: MI heart failure

pda 1 (11 decks)

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