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Pharma Downloads Pharma Downloads: 1-Clinodin 2-Guanbenz 3-Guanfacine

Centrally acting alpha2 adrenergic agonists like clonidine and guanfacine are used to treat essential hypertension and manage severe hypertension. They work by stimulating the alpha2 receptors in the vasomotor center of the brain stem, which inhibits sympathetic outflow and increases parasympathetic activity. This decreases blood pressure. Common side effects include dry mouth, sedation, constipation, and postural hypotension. Methyldopa, an adrenergic blocking agent, is also used to treat essential hypertension, especially in pregnant women. It works by stimulating presynaptic alpha2 receptors and acting as a false neurotransmitter. Reserpine, guanethidine, and prazosin are other adrener

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100% found this document useful (1 vote)
255 views5 pages

Pharma Downloads Pharma Downloads: 1-Clinodin 2-Guanbenz 3-Guanfacine

Centrally acting alpha2 adrenergic agonists like clonidine and guanfacine are used to treat essential hypertension and manage severe hypertension. They work by stimulating the alpha2 receptors in the vasomotor center of the brain stem, which inhibits sympathetic outflow and increases parasympathetic activity. This decreases blood pressure. Common side effects include dry mouth, sedation, constipation, and postural hypotension. Methyldopa, an adrenergic blocking agent, is also used to treat essential hypertension, especially in pregnant women. It works by stimulating presynaptic alpha2 receptors and acting as a false neurotransmitter. Reserpine, guanethidine, and prazosin are other adrener

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Srihari Divya
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© © All Rights Reserved
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Drugs Selectivity Uses Mechanism of Action Side effect (toxisty))

-stimulation of alpha2 -bradycardia.


adrenergic receptor in
-drymouth
vasomotor center of brain -sedation.
1-clinodin Centrally acting -Treatment of
steam. -fluid & Na retentio
on , constipation.
2-Guanbenz alpha2 adrenergic essential HTN.
-inhibition of sympathetic -postural hypotensioion.
3-Guanfacine agonist. -management of
activity. -sudden withdrawal al can result in hypertensive crisis, nervousness,
sever HTN or rennin
-predominance of insomnia.
dependent HTN
parasympathetic activity.
Centrally active

decrease SNS bradycardia.


(sympathetic outflow from -dry mouth, edema. a.
vasopressor centers of -unpleasant sedation
ion (vertigo)
(
Metabolite of a- brain steam. -constipation.
methyl NE that -treatment of - a-methyl NE weaker than -postural hypotensio ion.
stimulate essential HTN. NE in certain vascular beds -hemolytic anemia.
ia. -drug fever, liver damage.
4-methyldopa
presynaptic - in hypertension (renal) Idiosyncratic reaction
ion
alpha2 pregnant women , -false-transmitter released -lactation(high prolactin
lactin in plasma)
adrenergic. high rennin, renal instead of NE so less -exterpyramidal sig
igns, nightmares , psychic depression
insufficiency.- vasoconstriction is -sudden withdrawal al can result rebound hypertensive .
produce. -drug & metabolitess interfere with catecholamine's.- Ejaculatory
failure
-unpleasant sedation
ion & lethargy & nightmares dreams.
-exterpyramidal sig
igns.
Adrenergic blocking

-increase tone, moti


otility & secretions of GIT with abdominal cramps,
1-Reserpine -
- Antihypertensive diarrhea & increasee acid secretion.
agent

agent -bradycardia, miosiss, nasal congestion, flushing, orthostatic (postural


hypotension.
postural hypotension
ion ((sever), dizziness, weakness.
2-Guanethidine Moderately sever
- Selective -intestinal crampingg & diarrhea.
3-Guandrel hypertension
-Ejaculatory failure,, edema, nasal congestion.
st
-treatment of -no block of a2 -1 dose produce hypotension.
hyp
alpha1
Adrenergic receptor

1-alpha1 adrenergic

prazosin essential HTN. receptor>>no reflex of - dizziness, weaknes


kness, headache.
receptor blocker -CHF>>decrease
Others (phetolamine tachycardia. -decrease LDL\HDL.DL.
antagonist

on vascular
blockers

& afterload & preload. -block a1 that control - dry mouth, urinary
ary frequency,
fr lethargy, sexual dysfunction.
smooth -improve urine flow
phenoxybenzamine constriction of Bothe -nasal congestion.
muscle>>relaxing in elderly male with
& doxazosin & prostate & ureters. -nightmares.- postuural hypotension.
bl. Ves. benign prostatic
terazosin) -salt &water retenti
tention.
>>lowering BP. hyperplasia.

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drugs selectivity Drug agent Uses Mechanism of action Side effect (toxisty)

B1 blocker -HTN. HTN: -heart failure.


Atenolol - HTN & Antiangina
-HTN in young patient. -action appear after 4 weeks. -rebound phenomenon
Betaxolol Antiangina -in high rennin & HTN -decrease rennin& level of angiotnsion2. (angina,arrhythmia, MI HTN,)
with angina or -decrease NE & sympathetic flow from CNS -exacerbation of asthmatic
acebutolo Antiangina
carioselective

arrythemia. (presynabtic B receptor blocked). symptom.


HF -ischemic heart -cardioprotective &antagonize tachycardia -Hypotension A.V. block in patint
bisoprolol B1 blocker
disease, angina induced by other hypotension drugs. reciving Ca channel blocker.
Very short antiarrhythmtic pectoris. -↓ blood pressure. -detrimental diabetics dut to 2
Esmolol -CHF, migraines. action
acting
-most be withdrawn Heart failure: 1- tachycardia>>signals
-HTN & gradually to avoid -↑catecolamins. hypoglycemia.
metoprolol B1 blocker
antiarrhythmia angina or infraction -upregulation of B-receptors. 2-suppression of glycogenolysis.
- -HTN & -supraventicular & -↓HF.↓ remodeling block catecholamine. -exaggerated & mask hypoglycemic
antiarrhythmia ventricular -prevent of cardiac arrhythmia. action of insulin or oral
Adrenergic receptor blockers

2-beta adrenergic antagonist

-use with arrythemias. -antagnoisem of ventricular wall stress hypoglycemic.


propranolol Non selective
vasodilators r to .-mild & moderate HF. caused by sympathetic overactivity. -↓ hepatic blood flow &produce
prevent reflex of -↓mortility & hosplition non specific enzyme inhibition.
tachycardia. in HF. Antiarrythmia: -elevated triglyceride & decrese
--HTN & -Patient of MI & -↓slop of p4 depolarization slwing heart. HDL-cholestrol.
antiarrhythmia HF>>most take long -↓automaticity. -decrease exercize tolerance>>mild
Pindolol Non selective -Partial agonist (less term treatment. -dealy AV conduction. chronic fatigue.
bradycardia than ↑AV nodal refraction>>help in terminate -sedation
Non cardio selective

other beta blocker) nodal reentrant arrhythmia. -nightmares.


sotalol antiarrhythmtic -contractility diminished. -depression , vivd dreams &
timolol Antiangina impotence.
penbutolol Antiangina Antiangina: -intermittent claudation & cold
carteolol Antiangina --ve chronotropic & inotropic & ↓ aftrload. extremities.
-↓ myocardial O2 consumptionm Carvedilol & labetolol:
- HTN & Antiangina
especially during exersize. Orthostatic HTN due to a1.
Nadolol Non selective Long half life (better
-↓ heart rate, force of myocardial -sexual dysfunction.
patient compliance)
contraction, CO, velocity of contraction. -liver injury by labetelol.
HTN & HF & -HTN with -protect cardiomyocyte from O2 free
Carvedilol B1 & a2 blocker -paresthesias (scalp tingling)
Antiangina pheochromocytoma. radicals formed during ischemic episodes.
-a 1receptor blocked -labetalol metabolite: false positive
B1 & a2 blocker -improve perfusion of subendocardium by for phyochromcytoma.
result vasodilatation. increasing diastolic perfusion time.
& -reductiot of HR by B1.
labetolol HTN & Antiangina
sympatholetic -Labtelol dose't alter
to B2 serum lipids.

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Drugs selectivity Drug agent Uses Mechanism of action Adverse effect

Antiangina & -orally active. Antiarrhythemia: verapamil & Diltiazem:


1-Amilodipin st
-exhibit high 1 pass -slow conduction by AV node &↓ slow of P4 -depression cont. &HF, ↓CO
antihypertensive
metabolism & high protine depolarization & ↓ cardiac contractility. -bradycardia & AV block, cardiac arrest &
Antiangina & binding. -dihydropyridines don't effect the atrioventricular constipation , hypotension, edema,
2-Felodipin
antihypertensive -active after 30 min & have conduction sys. & sinoatrial node at normal indigestion & reflux oseophagitis.
plasma half live of several dose>>don't have direct effect on conduction or -short acting dihydropyridines have
vascular selective

dihydropyridines 3-Nimodipine
Dihdropyridines

Antiangina & hour (24-50hr) automaticity. associated with ↑ sympathetic tone .


(selective to
antihypertensive -exerted as metabolite in
st
-Bioavilability is ↓ because of 1 pass hepatic -long acting safe in treat HTN
cerebral ves)
urine. metabolism.
Antiangina & -↓myocardial O2 -longer half life lives for elderly patints &npatints minor toxicity ( dihydropyridines):
4-Isradipine
antihypertensive consumption by: with hepatic cirrhosis or renal insufficiency. -hypotension, headach, dizziness, edema &
5-Nicardipine Antiangina & 1-↓afterload (aortic flushing due to excessive dilatation.
pressure). Antihypertensive: -aggrevating of myocardial ischemia due to
(coronary ves) antihypertensive
2- verapamil ↓HR & -↓preiphral resistance. reflex tachycardia resulting from
Antiangina & contractility except -interfeare with angiotension2 & a1 mediated hypotension.
6-Nifedipine antihypertensive dihydropyridines which vasoconstriction. st
-short acting should not be used as 1 line to
& antiarrhytmaia have minimal effect -no effect on venues bed>>no effect on preload treat HTN but long acting such as amilodipin
(↓bp,↑HR & COP) >>vent. Filling pressure. appear safe.
-littile or no effect on non vascular smoothe cell
Ca channel blocker

-improve O2 delivary to
diarylaminopropylamine
(arterio-dilator)

ischemic myocardium by (tracheal). -Bepridil :


vasodilators of coronary -T-type regulating Ca influxin pacemaker cells & can prolong AP. & cause torsades de pointes
Antiangina & arterioles & ↓ HR (↑time cell of conduction sys. arrhytmia (drug induced long QT syndrome).
7-Bepridil spent in diastole) -↓CVR & ↑ coronary blood flow.
antihypertensive
-may inhibit platlet - Non- Dihdropyridines inhibt liver enzyme. - verapamil :
aggregation. may ↑ serum digoxin level in digitalized
patient.
Non- Dihdropyridines

Antiangina: -IV administration most contraindicated wih


cardiac selective

-block voltage sensitive Ca channel. beta blocker due to the possibility of AV


-all block L-type Ca channel which are aboundent block or sever depression of ventricular
Benzothiazipines

in cariomyocyte,arteriole smoothe muscle cell, SA function.


Antiangina & nodal tisse & AVnoda tissue.
8-Diltiazem antihypertensive -bepridil block Na & K channel that blocking -Non- Dihdropyridines can worsen cardiac in
& antiarrhytmaia activity in the heart>>prolong cardiac patint with HF.
repolarization. -in patint
-dihydropyridines reflex ↑ in sympathetic tone (
-IV administration for inotropic, chronotropic) due to ↓ arterial pressure,
phenylalkylamins

interrupting can ↑ HR & contractility which may aggravate


Antiangina & supraventricular angina.
9-verapamil antihypertensive arryhtemias. -Non- Dihdropyridines drug have direct –ve
& antiarrhytmaia inotropic, chronotropic & dromotropic effect.

Pharma Downloads
drugs Drug agent Treatment of Act on Mechanism of action Uses Take it with Side effect (toxisty)
--decrease Na & Cl
r
reabsorbtion. -mild to moderate hypertension & normal cardia
iac/ -fixed dose with -hypokalemia.
-
-decrease PVR. renal function. potassium sparing & -impaired diabetic
hydrochorothiazide, Distal -
-promote Ca reabsorbtion. other hypertensive control.
hypertension
chlorothaliadone tubule -
-potassium lose in exchange drug. -Hyperuricemia.
-not useful in renal insufficiency (glom filtration
n
THIAZIDE

m
mechanism. -combination with -muscle cramps.
-
-direct arteriolar vasodilators rate less than 40 ml/min). vasodilators drug . -increase LDL\HDL.
aff
affect.
hypertension
and edema -vasodilators diuretic .
Distal
Indapamide caused by
tubule
congestive
heart failure

Edema (fluied retention) associated with heart


-ototoxicity
+ + - failure.
--inhibitors of Na -K -2Cl (furosemise).
Use supplemental
in the s
symporter. - furosemise &
hepatic cirrhosis potassium , ACEIs or
thick -
-decrease circulatory volume. ethacrynic acid block
potassium sparing
Loop diuretic

furosemise & ascending -


-decrease preload & edema. renal excretion of uric
Hypertension diuretic to prevent
ethacrynic limb of -
-increase urinary Ca in useful in renal insufficiency (glom filtration rate acid.
& heart potassium depletion.
acid,Bumetanide,torse the loop co
constant to action of thiazide. less than 40 ml/min ,nephrotic syndrome. -potassium depletion.
failure Use different side of
mide of Henle -
-increase renal blood flow by -hyperglycemia &
diuretic in patient not
(high de
decrease RVR. hypertension hyperlipidemia.
response to oral
ceiling) -
-veno dilators through PG -dehydration.
diuretic
p
pathway. -shorter duration of
cerebral/pulmonary edema where rapid diuresis is
required (IV injection). action.

- to avoid potassium depletion in patint takingg


--Spironolactone antagonize digitalis. Hyperkalemia &
e
effect of aldosteron. -combination with other diuretic to prevent effeect gynecomastia.
Potassium sparing

hypertension of hypokalemia).
amiloride, and
spironolactone & management
Triamterene. of congestive
heart failure. - amiloride& Triamterene Amiloride inhibit smooth muscle response to Hyperkalemia &
d
don't antagonize effect of contraction (effect in trans-membrane & gastrointestinal -
al
aldosteron. interacellular Ca movement). distribances.

Pharma Downloads
drugs Treatment of Vasodilators of Mechanism of action Uses Take it with Side effect (toxisty)
Hydralazine HTN & HF. dilate resistance 1-direct effects on the vascular Hypertension: used in -headaches, edema ,paresthesias, flushing
(apresoline) vessels (arterial smooth muscle (dilation). conjunction with tachycardia.
dilators) 2- highly specific for arterial 1- arterial HTN a beta-blocker -precipitate angina in patients with coronary artery
vessels greater than viens. 2- acute HTN emergencies. (propranolol) and disease.
3- reduces total periphral 3- secondary HTN . thiazide diuretic -lupus-like syndrome.
resistance and arterial 4- pulmonary HTN to attenuate the
pressure. baroreceptor-
4- increase cardiac work & mediated reflex
Heart failure:
decrease afterload. tachycardia and
5-Indirect cardiac stimulation sodium retention,
(e.g., tachycardia) due to 1- management of chronic respectively.
activation of the baroreceptor heart failure because of
reflex. its ability to reduce
6-salt and water retention due afterloadand thereby
to reflex of stimulation of RAS. enhance stroke volume
and ejection fraction.

minoxidil HTN & HF. dilate resistance Open K channels in smoothe 1- HTN emergencies. used in -Tachycardia, palpitation, angina , edema, fluied
vessels (arterial muscle membrane. 2- treatment of male- conjunction with retention, nausea, vomiting, flushing, headache,
dilators) pattern baldness. a beta-blocker sweating.
and diuretic -hypertrichosis.
diazoxide HTN arterial dilator 1-IV infusion. 1- HTN emergencies>>long Used (hyperstat) -sever Tachycardia, prolonged hypotension, nausea ,
2-activation of ATP sensitive duration of action. infusion pumps vomiting . salt & water retention,
potassium channel. 2- Hypoglycemia. are unavailable. -hyperglycemia due to inhibit insulin release and can
3-hyperpolarization of cause diabetes.
arteriolar smoothe muscle.
4-rapid fall of TPR >>reflex
tachycardia.
fenoldopam HTN Dilation of Agonist at dopamine D1 1- HTN emergencies. Given continous Tachycardia, palpitation, headache.
peripheral receptor. IV infusion -Increase intraorpital pressure so avoided in
arterioles and glaucoma.
naturesis.
Prazosin HTN & HF. Arteriolar & venous. Block of alpha1 adrenergic 1- HYPERTENSION.
receptor. 2- Raynaud's disease.
ACEIs HTN & HF. Arteriolar & venous. Inhibit ACE & decrease AII 1- HTN CHF.
Nitroglycerin CHF & angina venous Produce No increase cGMP. 1- Raynaud's disease
pectoris 2- CHF & angina pectoris
Na HTN & HF. Arteriolar & venous. Produce No increase cGMP. 1- Acute CHF Take with beta- Due to vasodilatation : hypotension , nausea ,
nitroprosside 2- HTN emergency blocker because vomiting , muscle twitching , methemoglobinemia ,
tachycardia of reflex toxicity , arrhethmei

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