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Pharmacology Summary

Pharmacology Summary

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Published by sechzhen

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Published by: sechzhen on Nov 13, 2009
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DRUGEXAMPLESUSESMECHANISMSIDE EFFECTSACE inhibitors
Ramipril,Lisinopril
Hypertension
Heart Failure
Post MIBlock ATI
ATII by binding tothe site on the enzyme thatnormally accommodates theterminal leucine of ATI.
Inhibits vasoconstriction.
Hypotension
Dry cough(increasedbradykinin)
Renal failure in ptswith bilateral renalstenosis
Beta-Blockers
Atenolol,Propanolol
Hypertension
Angina
Arrhythmias
Stable heart failureblock
β
-adrenergic receptors inhibitingtheeffects of adrenaline and nonadrenaline.
β
1 (heart) blockage
decreases HRandcontractility
,
β
2 (bronchial andvascularsmooth muscle) blockage causes
vasodilation
.
Provocation of asthma, heartfailure.
Cold hands
Bradycardia -fatigue
CalciumChannelBlockersDihydropines
Amlodipine,
Phenyalkylamines
-Verapamil,
Benzthiazepines
-Diltiazem
Hypertension
Angina
Supraventriculararrhythmia –(Phenylalkylaminesonly)
Vasodilation
block cellular entry of Ca
+
bypreventing opening of voltage-gated L-type and T-type calcium channels
Flushing, headache,
P.oedema
Phenyalkylamines –can worsen heartfailure
Gynaecomastia
Impotence
ThiazideDiuretics
Bendrofluazide,hydrochlorothiazide
Hypertension
Combined with loopfor Heart Failureincrease water excretion bydecreasing reabsorption of Na
+
and Cl
-
in the distaltubule by binding to the Cl
-
site of the electroneutralNa
+
/Cl
-
co-transport systemand inhibiting its actioncausing a decrease in bloodvolume, venous return andCO
Hypokalaemia
Hyponatraemia
Hypotension
Gout
 Type II DM
Loop Diuretics
Frusemide,Bumetanide
Hypertension (butless effective thanthiazides – usedwhen renalimpairment orresistant to multipledrug Tx)
Heart FailureBlock Na
+
resorption inascending loop of Henle –diuretic effect.
Hypokalaemia
Hyponatraemia
Hypotension
Gout
Potassium-sparingdiuretics
Spironolactone,Amiloride
SecondaryHypertension
Severe heart FailureBlocks action of aldosteronein distal convoluted tubule –diuretic effect
Hypokalaemia
Hyponatraemia
Abdominaldiscomfort
 
Angiotensin IIreceptorantagonists
Losarten,Valsarten
Hypertension
Alternative to ACEinhibitor in heartfailure
Vasodilation
– by inhibitionat the angiotensin II receptor
Usually mild
No cough like inACE inhibitors
Alpha-adrenoreceptor antagonists
Doxazosin,Prazosin
Hypertension (inaddition to otherhypertensives)Reduces peripheralresistance by inhibiting
α
1
-adrenoreceptor-mediatedvasoconstriction.
PosturalHypotension
Dizziness
 
Fibrinolytics
Streptokinase
 Thrombolysis –Acute MI, stroke, PEForms a complex with, andactivates, plasminogen intoplasmin.
Nausea/vomiting
Bleeding
Antiplatelet agentsAsprin
Prevention andtreatment of MI andstroke.Irreversibly inhibits COX andso stops synthesis of  Thromboxane A
2
fromArachidonic Acid which leadsto
platelet aggregation.
Haemorrhage
Clopidogrel
Prevention andtreatment of MI andstroke.Inhibits activation of theglycoprotein IIb/IIIa receptoron the surface of plateletswhich is required foraggregation to occur.
Haemorrhage
AnticoagulantsWarfarin
Prophylaxis+treatment DVT, PEProphylaxis of embolization in AF,Rheumatic disease +prosthetic valves.Blocks reduction of Vit. K epoxide
necessary forsynthesis of factors II, VII, IXand X.
Haemorrhage
Heparin
 Treatment of DVT,PE. Prophylaxis of DVT/PE post op.
MI.Activates antithrombin III,which limits blood clotting byinactivating thrombin andfactor X.
Haemorrhage
Statins
Atorvastatin,Simvastatin,Pravastatin
Prevention of cardiovasculardiseaseReversibly inhibit enzymeHMG CoA reductase whichcatalyses the rate-limitingstep in the synthesis of cholesterol:HMG CoA
mevalonicacid
cholesterol. This
in synthesis
LDLreceptors so
LDL levels.
Myopathy (muscleache)
Disturbed LFTs
Abdominal pain
Nitrates
Glyceral trinitrate(GTN), Isosorbidemononitrate
Prophylaxis and Treatment of angina.
LVFProdrugs – they decomposeto form NO which activatesguanylyl cyclase, thereby
cyclic guanosinemonophosphate (cGMP).Protein kinase G is activatedand contractile proteins arephosphorylated. This allleads to Dilation of vessels.
Posturalhypotension
 Tachycardia
Headache
Flushing
Dizziness
Potassiumchannelactivators
Nicorandil (onlylicensed one)
Prophylaxis of anginaRelaxation of smooth muscleand vasodilation.Activates K 
+
channels of vascular smooth muscle
Headache

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