Drugs And Actions Flashcards
*Atropine
**nonselective muscarinic antagonist **
blocks Ach peripheral and centrally.
cardiovascular –> M2–> cAMP increases–> contraction and CO
–> Emergencies in surgery to increase heart rate/before GA
dry mouth, constipation, headaches
increase hypertension
increase or decrease anti collinergic effects
Benzatropine
M1 muscarinic antagonist
Inhibits ach –> inhibits dopamine reuptake
= Parkinson
dry mouth, constipation, headaches
increase hypertension
increase or decrease anti collinergic effects
*Perindopril
ACE inhibitor
prevent conversion AGTI –>AGTII (vasocontriction)
=Hypertension / heart failure
cough, dizziness, postural HYPOtension
triple whammy + diuretic + NSAIDs –> renal failure
*Losartan
ARB
specific to smooth muscle wall = Angiotensin receptor blocker
Vasodilation
=hypertension
Xerostomia, dizziness, postural HYPOtension
triple whammy + diuretic + NSAIDs –> renal failure
*Frusemide
loop diuretic
inhibits cotransporter NA-K-CL –> inhibits Na, Cl, K reabsorption = more urine excreted
= hypertension –>decrease blood (plasma) volume
= heart failure
Xerostomia, dehyration, Postural hypotension
triple whammy + diuretic + NSAIDs –> renal failure
*Indapamide
Thiazide diuretic
Inhibits Na+ & Cl- retuptake in the distal tubule, reduced osmotic pressure, increasing urinary output, Lowering blood volume = lower Cardiac output (CO)
=Hypertension
Xerostomia, dehydration
triple whammy + diuretic + NSAIDs –> renal failure
Spironolactone
K sparing diuretic
Antagonizes aldosterone at the distal tubule
A weak diuretic: inhibit Na+ reuptake, hence makes the kidney pass out more fluid whilst retaining/increasing potassium by inhibiting the exchange between Na and K
=MAnagement of odema from heartfailure
weak –> hypertension
Hyperkalemia, Xerostomia, dehydration, menstrual abnormalities
triple whammy + diuretic + NSAIDs –> renal failure
*Amlodipine
Calcium channel blocker
. Vascular smooth muscle selective = dihydropyridines
Vasodilator
=hypertension
Gingival hyperplasia, xerostomia, dizziness, taste disturbances
CYP interaction
(erytheromycin or miconazole-treats thrush)
Darifenacin
Anti muscarinic antagonist
M3: Smooth muscle (bladder)
relaxes detruser muscle of the bladder
=*urinary incontenance *
Xerostomis, constipation, headaches, tachycardia
*Atenolol
B1 antagonist (B blockers)
Prevents NE/E from binding to B-adrenergic receptors in SA node
Decrease contraction (-ve inotropic effects),
decreased HR (-ve chronotropic effects)
decrease SV= decrease CO = decrease BP
=hypertension
fatigue, postural hypotension, dizziness
cardiac depression with GA, NSAIDS = antagonist to B blockers,
Digoxin
NA/K ATPase
ATPase = controls movement of Ca, Na and K in heart. Increase intracellular Ca and Na Increase cardiac contractility > increase cardiac output
Increase strength/efficiency heart contractions
=Heart failure, AF
Weakness, dizziness, SOB, nausea, vomiting
Verapamil = toxicity due to heapatic metabolism
*Glyceryl Trinitrate (GTN)
Nitrate
stimulates guanylate cyclase in smooth muscles by decreasing Ca and vascular tone > venodilation
Reduction in CO and arterial pressure reduces the O2 demand by the myocardium + dilation of coronary and coronary collateral vessels increases coronary perfusion and oxygen delivery
=Angina
Xerostomia, Dizziness, Syncope, headaches, postural hypotension
PDE5 inhibitors (e.g. Sildenafil-excessive hypotension)
Amiodarone
K inhibitor = Anti-arrhythmic
* Blocks certain electrical signals in the heart
* Can block K, Na, C and B receptors. Has the potential to cause a variety of complex effects in the heart
* =Ventricular fibrillation, Tachycardia
Metallic taste, skin rash, pulmonary fibrosis, GI and CNS disturbances
CYP interaction
(erytheromycin or miconazole-treats thrush)
Digoxin: CYP interactions
Flecainide
Na inhibitor = Anti-arrhythmic
Suppresses premature ventricular contractions
* QT elongation
* = ventricular tachycardia, AF, dysrhythmias*
Xerostomia
*Diltiazem
non-dihydropyradines = Cardiac specific
Calcium channel blockers
reduce HR and cardiac contractility
* =Arrythmias
Gingival hyperplasia Orthostatic Hypotension DizzinessTaste disturba
*Atorvastatin
HMG-CoA reductase inhibitor
inhibits synthesis of cholesteroal through liver enzyme HMG-CoA reductase –> reduce LDL’s
Lowers LDL and TG and raise HDL
* Dyslipidaemia
Dizziness
CYP interaction
(erytheromycin or miconazole-treats thrush)
*Fenofibrate
PPAR-alpha agonist
Increase lipolysis; decrease TG
Lowers TG, LDL and raise HDL
* severe hypertriglyceridemia
* mixed hyperlipidaemia
Dizziness, nausea, constipation
*Aspirin
Anti platelet Thromboxane synthesis inhibitor
Blocks COX-1 = thromboxane A2 (aggregatior).
Prevent platelet aggregation
Blocks COX-2: prostaglandins (promote pain, inflammation, fever, also cause platelets to stick together and form a blood clot, protection of stomach from acid
* = Thromboembolism, Heart attack, stroke, pain, inflammation
GI issues (pain ulcerations), KI/LR failure, bleeding
Warfarin (stomach bleeding)
Anti-thrombotics (bleeding risk)
SSRIs & NSAIDS (bleeding risk)
Antihypertensives (increase BP- physiological antagonists)
Diuretics (reduce effect)
*Clopidogrel
Anti-platelet
P2Y12 inhibitor
Prevents platelet aggregation/thromboxane production
Decreased clots formed = stroke & Heart attack
Taste disturbance
Grape juice: can increase side effects
*Dabigatran
Anti Coagulant
Blocks cleavage of fibrinogen (I) into fibrin (Ia); activation of platelets, and clot formation
= DVT, stroke
Bleeding from gums
Antiplatelet
NSAIDs
*Warfarin
Anti Coagulant
Vitamin K antagonist
=Myocardial infarction
Pulmonary embolism
Strokes
Atrial fibrillation
Venous thrombosis
Thromboembolism
Dizziness, headache, weakness, bleeding gums
Increased bleeding risk:
Anti-coagulants
Direct thrombin inhibitors
Antiplatelets
NSAIDs
SSRI’s (e.g. sertraline)
Antibiotics (e.g. erythromycin)
Antifungals (e.g. miconazole)
CYP450 enzyme drugs (e.g. amiodarone, erythromycin, miconazole, metronidazole)
*Enoxaparin
Anti Coagulant
Inhibits factor Xfactors Xa and IIa. Factor Xa catalyzes the conversion of prothrombin to thrombin
=Stroke, DVT
Nausea, Diarrhoea, fever
NSAIDs
Anticoagulants
*Rivaroxaban
Anti Coagulant
Inhibits free and clot bound factor Xa- needed to activate prothrombin (factor II) to thrombin (factor IIa).
One molecule of factor Xa can generate more than 1000 molecules of thrombin
The action is irreversible
Bleeding gums, Dizziness, Headache, Coughing up blood
Antiplatelet
NSAIDs
*Tranexamic acid
Anti-fibrinolytic
Inhibits activation of plasminogen
= Reduce/prevent hemorrhage during and following tooth extraction
=Haemophilia (short term use- 2-8 days)
Hoarseness, Swelling of face
Difficulty breathing/swallowing
Caution in
