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101 Cards in this Set

  • Front
  • Back

what is epinephrine

A potent vasoconstrictor and cardiac stimulant.

The rise in systolic blood pressure that occurs after epinephrine is due to what

positive inotropic and chronotropic actions on the heart (predominantly β1receptors)


and the vasoconstriction induced in many vascular beds (a1receptors).

Epinephrine also activates what

β2 receptors in skeletal muscle blood vessels

this activation causes what

dilation

how does epinephrine affect exercise

contributes to increased blood flow

Norepinephrine acts of which receptors

alpha and beta

NE acts more on which receptor

alpha

Norepinephrine _______peripheral resistance and both diastolic and systolic blood pressure

increases

NE has _______inotropic effects on the heart

positive

Phenylephrine acts mostly on which receptors

a1 receptors

Phenylephrinedoes does what to TPR

increases

Phenylephrine does what to venous capacitance

decreases

acts on what receptors in the iris?


causes what effect?

alpha 1


mydriasis

does what to blood pressure

increases systolic and diastolic

acts on what receptors in the nasal mucosa?


causes what effect?

alpha 1


decongestion

what isIsoproterenol (isoprenaline)

Potent β-receptor agonist

does it affect alpha receptors

little effect

what type of chronotropic and inotropic action? why?

positive


because it activates β receptors almost exclusively. it is a potent vasodilator.

what happens to cardiac output and BP

CO increases and diastolic and mean arterial pressure decreases

dopamine activates which receptors


and leads to what?

D1 receptors


vasodilation

does dopamine act on dose dependent receptors?

yes

at low doses, dopamine acts on which receptors? this causes what?

dopaminergic receptors


increased renal, coronary, and cerebral blood flow.

at what fusion rate does dopamine act on dopaminergic receptors

2 to 5 mcg/kg/min

when does dopamine begin to act on β receptors?


what happens?

5mcg/kg/min


increase in cardiac contractility and heart rate

when does dopamine begin to act at a-receptors in the periphery?


what level of dosage is it considered to be?

10 to 20 mcg/kg/min


high

what is Dobutamine

relatively β1-selective syntheticcate cholamine

does Amphetamine readily enters the CNS

yes

what does it affect

stimulant effect on mood and alertness and a depressant effect on appetite

Its peripheral actions are mediated primarily through the release of what

catecholamines

what differentiates Methamphetamine(N-methylamphetamine) from amphetamine?

Meth has higher ratio of central to peripheral actions

what is Ephedrine? what does it do?

mild stimulant


Displaces NE from storage vesicles in presynaptic neurons

what is Pseudoephedrine

OTC component of many decongestant mixtures

what are Xylometazoline and Oxymetazoline

Directly-acting a agonists

what are these drugs used for and why

used as topical decongestants because of their ability to promote constriction of the blood vessels of the nasal mucosa

what is Rhinitis medicamentosa

rebound nasal congestion due to down regulation of alpha receptors

what does it do

decreased endogenous norepinephrine production, etc

2 types of a2 Selective Agonists

Clonidine and Apraclonidine

what is clonidine used for

Used in hypertension, diabetic diarrhea,narcotic addicts and to treat benzodiazepine withdrawal effects

what are its side effects

Postural hypotension, dry mouth, sedation, rebound hypertension

what is Apraclonidine


what is it used for

A clonidine derivative


Used in glaucoma

what is Cocaine

local anesthetic with a peripheral sympathomimetic action

whats its action from

inhibition of transmitter reuptake at noradrenergic synapses

does it readily enter the CNS?


what does it produce?

yes


amphetamine - like effect that is shorter lasting and more intense.

the major action of cocaine on the CNS is to what

inhibit dopamine reuptake

what is Tyramine

normal by-product of tyrosine metabolism in the body

where is it also found

in high concentrations in fermented foods such as cheese

what happens if administered parenterally

it has an indirect sympathomimetic action caused by the release of stored catecholamines

its spectrum of action is similar to what

NE

when is the effect of tyramine is greatly intensified

In patients treated with MAO inhibitors (particularly MAO-A isoform)

who must avoid tyramine containing foods

Patients taking MAO inhibitors

Increased sympathetic system activity can lead to what

pathological conditions

Blockade of SNS can provide beneficial effect when______

there is increased SNS activity

Receptor specific blockers _______ the unwanted side effects associated with these blockers

decreases

3 types of adrenergic drugs

Alphablockers


Betablockers


Alphaplus beta blockers

2 types of alpha blockers

Phenoxybenzamine


Phentolamine

Phenoxybenzamine blocks what

blocks α1> α2

is it reversible or irreversible

Irreversible,forms covalent bond with receptors

Phentolamine blocks what

blocks α1= α2

is it reversible or irreversible

reversible

4 types of a1 selective blockers

•Prazosin


• Terazosin


• Doxazocin


• Tamsulocin

2 types of a2 selective blockers

Yohimbine


Mirtazapine

what is Mirtazapine used for

antidepressant

Alpha Blockers used for Pheochromocytoma

•Phenoxybenzamine / Phentolamine

Alpha Blockers used for essential HTN

Prazosin

alpha blockers used for Hypertension due to clonidine withdrawal

•phenoxybenzamine /Phentolamine.

which alpha blocker is used in Raynaud's Phenomenon

prazosin

which one is used in Benign prostatic hyperplasia (BPH)

a blockers- Prazosin


a1a blockers - Tamsulosin is preferred

how do they work

They decrease the tone of prostate/ bladder muscles

prostate has which receptors predominantly

a1a

bladder has which receptors

a1a receptor 1/3, a1d receptor 2/3

what happens in Benign Prostate Hyperplasia (BPH)

Overactive a1areceptors in bladder trigone,prostrate and prostatic urethra ­INCREASES smoothmuscle tone – urinary retention

Blockade of these receptors by what relaxesthese structures

tamsulosin or terazosin

alpha blockers do what to the bladder

Increase urinary flow rate-more complete emptying of the bladder

does it reverse the hyperplasia?

no

does it offer symptomatic relief

yes

best treatment for BPH

tamsulosin+ finasteride

what does finasteride do?

finasteride is5-α reductaseinhibitor - inhibits conversion of testosterone to more potent dihydrotestosterone

what is Yohimbine

a2 selective blocker

what does it do?


what are its potential uses?

Enhances sexual activity – aphrodisiac


Potential uses: postural hypotension and impotence

what is Mirtazapine

a2 blocker

what is it used for

used in depression

At higher doses, beta 1 selective drugs will also______

block beta 2 receptors

7 Non-selective β1 and β2 receptor blockers

carteolol


nadolol


penbutolol


pindolol


propranolol


sotalol


timolol

7 Selective β1 receptor blockers

atenolol


acebutolol


betaxolol


bisoprolol


esmolol


metoprolol


nebivolol

3 α and βreceptor blockers

Carvedilol


labetalol


bucindolol

the Beta blockade consists of what

b1 - Decreases HR, CO


b1 - Decreases renin release


b2 - Decreases aqueous humor production

6 b1 (Cardioselective) blockers


(ABEAMN)

•Atenolol


•Betaxolol, bisoprolol


•Esmolol


•Acebutolol(with ISA)


•Metoprolol


•Nebivolol

which one has a short half life of 10 minutes

Esmolol

advantages of b1 (Cardioselective) blockers

safer in bronchial asthma, diabetes mellitus and peripheral vascular diseases

clinical uses of Nonselective Beta Blockers

•Hypertension


•Angina


•Migraine headache


•Cardiac arrhythmia


•Glaucoma


•Myocardial infarction


•Essential tremors


•Congestive cardiac failure


•Hyperthyroidism


•Stage fright / Performance anxiety

how are Nonselective Beta Blockers in MI's

prevents reinfarction and improves long term survival

which one is used in CHF

carvedilol

which one is used in glaucoma

timolol

most common adverse effect of beta blockers

bradycardia (inhibits AV conduction. If HR<60, should not use βblockers)

chronic use of beta blockers is associated with what

raised lipid levels (LDL andTG)---- mechanism unknown

other adverse effects of beta blockers

Weakness/Fatigue


Hypotension


hallucinations


Impotence


CHF


Masks symptoms of hypoglycemia


May cause hypoglycemia (decreases glycogenolysis)or hyperglycemia (inhibits insulin secretion).

beta blocker overdose can lead to what

severe cardiac failure in susceptible individuals


topical application can lead to toxicity

antidote for beta blocker overdose

glucagon

what does it do

binds to glucagon receptor - activates adenylyl cyclase - increases cAMP, and has inotropic and chronotropic effects on heart

3 Non-Selective Beta Blockers Contraindications

bronchial asthma


prinzmetal angina & peripheral vascular disease


diabetes mellitus

Raynaud’s disease and Prinzmetal angina first drug of choice

calcium channel blockers