drug therapy of the muscular system

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    I. DRUG THERAPY OF THE MUSCULAR SYSTEM:

    A. CENTRALLY ACTING SKELETAL MUSCLE RELAXANT:

    Actions: exact mechanism of action is still unknown, except that they act by CNSdepression. All of these muscle relaxants produce some degree of sedation &

    most physicians believe that the benefits from these agents come from the

    sedative effect rather from the actual muscle relaxing effect

    Uses: for relief from muscle spasm (spinal cord injuries, rheumatic d/o)

    Side Effects: sedation, weakness, GIT upset

    Adverse effects: liver damage, blood dyscracias

    Drug interactions: Alcohol, narcotics, barbiturates, anticonvulsants, sedative

    hypnotics, tranquilizers and anti depressants can ENHANCE its depressive effect

    Agents: carisoprodol, chlorzoxazone, metaxalone, methocarbamol, tizanidine

    B. DIRECT ACTING SKELETAL MUSCLE RELAXANT; DANTROLENE

    Actions: this agent acts directly on skeletal muscles producing generalized mild

    weakness of skeletal muscles & decreases the force of reflex muscle contraction,hyperrelfexia, clonus, muscle stiffness, involuntary muscle movements &

    spasticity

    Uses: Cerebral palsy, multiple sclerosis, stroke syndrome, Malignant

    hyperthermia

    Side effects: weakness, diarrhea, drowsiness, dizziness

    Adverse effects: photosensitivity. Liver damage

    Drug interactions: CNS DPRESSANT: alcohol, analgesics, tranquilizers,potentiates the sedative effect of dantrolene

    C. NEUROMUSCULAR BLOCKING AGENTS:

    Actions: Acts by interrupting transmission of impulses from motor nerves of

    muscles at the NMJ. Neuromuscular blocking agents have no effect onconsciousness, memory or pain threshold

    Uses: used during induction of anesthesia, intubation and electroshock therapy

    Side effects: salivation, discomfort

    Adverse effects: signs of respiratory distress, diminished cough reflex, & inability

    to swallow

    Drug interactions: Drugs that enhance Therapeutic & toxic effect: anesthetics, theaminoglycosides, beta blockers, quinidine, diuretics.

    Agents: atracurium, cisatracurium, doxacurium, mivacurium, succinylcholine,

    tubocurarine Cl.

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    II. DRUGS AFFECTING THE CARDIOVASCULAR SYSTEM

    A. DRUGS USED TO TREAT HYPERLIPIDEMIAS:

    1. BILE ACID-BINDING RESIN: Actions: cholestyramine & colestipol are resins that bind bile acids in the

    intestines. After oral administration, the resin forms a non-absorbable complex

    with bile acids, preventing enterohepatic recirculation of the bile acid. Because ofthe removal of the bile acid, liver cells compensate by increasing metabolism of

    cholesterol to p[roduce more bile acids , resulting in the net reduction in total

    cholesterol levels

    Uses: used in conjunction with dietary therapy to decrease elevated cholesterol

    concentration, in type II hyperlipidemia. Also for treating pruritus in biliary stasis,

    diarrhea

    Side effects: constipation, bloating, fullness, nausea

    Adverse effects: Flatulence Drug interactions: digitoxin, warfarin, thyroxine, diuretics, Phenobarbital,

    NSAIDS, tetracyclines & beta blockers: reduces absorption. Bile acid binding

    agents reduces absorption of fat soluble vitamins

    2. NIACIN:

    Actions: this is also called nicotinic acid. A water soluble vitamin B. the exact

    mechanism of action is unknown, but it appears to inhibit the formation of VLDL

    which in turn lowers the LDL levels

    Uses: used in conjunction with dietary therapy to reduce cholesterolin type II, III,

    IV, & V hyperlipidemias

    Side effects: flushing, pruritus, headache, nausea, abdominal discomfort,dizziness, fatigue

    Adverse effect: myopathy, anorexia

    Drug interactions: Lovastatin if combined w/ niacin enhances the myopathic

    effect

    3. HMGCoA REDUCTASE INHIBITORS;

    Actions: also called statins. They competitively inhibit the enzyme responsible

    for converting HMG-CoA to mevalonatein the biosynthetic pathway to

    cholesterol in the liver. The reduction in liver cholesterol increases the removal of

    LDL from the circulating blood. These agents are more effective if administeredat night because peak of production of cholesterol during this period.

    Uses: For hypelipidemia/cholesterolemia

    Side effects: head ache, nausea, abdominal discomfort.

    Adverse effects: Myopathy, liver dysfunction

    Drug interactions: Cyclosporine, itra/keto/fluco nazoles, niacin, verapamil,

    eryhthromycin increases the incidence of myopathy. Ranitidine, omeprazole &cimetidine, increases statin levels

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    Agents: atorvastatin, fluvastatin, simvastatin, lovastatin

    4. FIBRIC ACID:

    Actions: exact action is unknown

    Uses: for hypertriglyceridemia. Fibric acids are not recommended in combination

    with statins due to the risk of rhabdomyolysis Side effects: nausea, diarrhea, abdominal discomfort, fatigue

    Adverse effects: myopathy, jaundice

    Drug interactions: enhanced Warfarin effect, enhanced insulin effect. Probenecidincreases its toxic effect

    B. DRUGS USED TO TREAT HYPERTENSION

    1. DIURETICS:

    Actions: causes volume depletion, sodium excretion, & vasodilatation of

    peripheral arterioles. It has 4 classes: (a.) carbonic anhydrase inhibitors, (b.)Thiazide & thiazide like agents, (c.) loop diuretics, (d.) potassium sparingdiuretics. These are the most commonly prescribed antihypertensive agents

    because it is proven to lower cardiovascular morbidity & mortality associated

    with hypertension

    Uses: antihypertensive.

    2. BETA BLOCKERS:

    SEE MIDTERM NOTES

    3. ANGIOTENSIN CONVERTING ENZYMES INHIBITORS (ACEI)

    Actions: these act by inhibiting angiotensin I converting enzyme (dipeptidyldipeptidase), the substance responsible for conversion of angiotensin I to

    angiotensin II

    Use: antihypertensive

    Side effects: nausea, dizziness, diarrhea

    Adverse effects: Orthostatic hypotension, facial edema, neutropenialiver damage,

    hyperkalemia, chronic cough, teratogenesis

    Drug interactions: lithium, digoxin, capsaicin reduces therapeutic effects

    Agents: captopril, enalapril, quinipril, ramipril

    4. ANGIOTENSIN II RECEPTOR ANTAGONISTS: (AT1receptor antagonist) Actions: binds to angiotensin II receptor sites, blocking the very potent

    vasoconstrictor.

    Uses: antihypertension

    Side effects: head ache, dyspepsia, diarrhea

    Adverse effects: orthostatic hypotension, may be a teratogenic agent,hyperkalemia

    Drug interactions: Enhanced effect with: diuretics, alcohol, beta blockers

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    Agents: candesartan, irbesartan, losartan, valsartan

    5. CALCIUM ION ANTAGONIST:

    Actions: inhibits the movement of calcium ions across a cell membrane, this

    results in fewer arrhythmias a slower rate of cardiac contraction & relaxation ofsmooth muscles of blood vessels, resulting in vasodilatation & reduced BP

    Uses: antihypertensive

    Side effects: syncope, hypotension

    Adverse effect: edema

    Drug interactions: enhanced effect with- alcohol, phenothiazines, beta blockers,

    histamine antagonists

    Agents: amlodipine, nifedipine, nicardipine, verapamil

    6. ALPHA 1 BLOCKING AGENTS:

    Actions: blocks post-sympathetic alpha1 adrenergic receptors to produce

    arteriolar & venous dilatation, reducing peripheral vascular resistance w/oreducing cardiac output or inducing a reflex tachycardia. These agents do not

    increase catecholamines therefore there is no increase in heart rate or myocardialoxygen consumption. Because of the presence of alpha 1 receptors in the prostate

    gland & bladder, TERAZOSIN & DOXAZIN are also able to reduce urinary

    outflow resistance in men with BPH.

    Uses: hypertension, BPH

    Side effects: headache drowsiness, tachycardia, fainting

    Adverse affects: lethargy

    Drug interactions: Enhanced effect with- diuretics, tranquilizers alcohol,

    barbiturates, antihistamines

    Agents: Doxazin, terazosin

    7. CENTRALLY ACTING ALPHA 2 ANTAGONISTS

    Actions: stimulates the alpha adrenergic receptors in the brain stem , resulting in areduced sympathetic outflow from the CNS with a decreased HR, & PVR,

    resulting in BP drop

    Uses: Antohypertensive

    Side effects: drowsiness, mouth dryness, dizziness

    Adverse effects: DEPRESSION

    Drug interaction: enhanced effect with- digitalis, guanethidine, barbiturates,

    tranquilizers, beta blockers Agents: Clonidine, methyldopa

    8. PERIPHERALLY ACTING ADRENERGIC ANTAGONISTS:

    Actions: causes release & subsequent depletion of NE from adrenergic nerve

    endings. This causes a relaxation of vascular smooth muscle which decreases TPR

    & venous return. A hypotensive effect results that is greater in the standing than

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    in the supine position. Heart rate is decreased & fluid retention occurs. Sedation

    occurs due to depletion of NE in the brain

    Uses: Hypertension

    Side effects: sedation

    Adverse effects: orthostatic hypotension, edema

    Drug interactions: Enhanced effect with- barbiturates, diuretics, tranquilizers,antihistamines, alcohol

    Agents: guanethedine, reserpine, guanadrel

    9. DIRECT VASODILATORS

    Actions: causes direct arteriolar smooth muscle relaxation resulting in a decreased

    PVR. The reduction in peripheral resistance causes a reflex increase in HR, CO,

    & renin release with sodium & water retention.

    Uses: for stage 2 & 3 hypertension, baldness

    Side effects: nausea, dizziness, tachycardia, fever, chills

    Adverse effects: myalgia, arthralgia, orthostatic hypotension

    Drug interactions: enhanced effect with- diuretics, alcohol, beta blockers

    Agents: minoxidil, hydralazine, nitroprusside sodium

    C. DRUGS USED FOR THE TREATMENT OF HEART FAILURE:

    1. DIGITALIS GLYCOSIDES: DIGOXIN

    Actions: derived from the foxglove plant, this agent increases the force ofcontraction & slows down the heart rate, reducing the conduction velocity &

    prolonging the refractory period at the AV node. The excat mechanism of action

    is unknown.

    Uses: heart failure

    Side effects: bradycardia, tachycardia, n/v

    Adverse effects: HypoK, HypoMg, HypoCa

    Drug interactions: Enhanced effect with- nifedipine, verapamil, antibiotics,

    betablockers

    Agents: digitoxin, digoxin

    2. PHOSPHODIESTERASE INHIBITORS:

    Actions: increases the force & velocity of myocardial contractions by inhibitingCAMP phosphodiesterase activity & increases cellular level of CAMP in heart

    muscles. It is also a vascular smooth muscle relaxantthat causes vasodilatation,

    reducing preload & after load

    Uses: for short term treatment of heart failure

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    Side effects: N/V, abdominal discomfort

    Adverse effects: arrhythmias, hypotension, thrombocytopenia, liver damage

    Drug interactions: digitalis & furosemide.

    Agents: amrinone, milrinone

    3. ANGIOTENSIN CONVERTING ENZYME INHIBITORS

    Actions: Reduces afterload & help reduce circulating blood volume by inhibitingthe secretion of aldosterone

    Uses: reduces BP & increases renal blood flow

    D. DRUGS USED TO TREAT ARRHYTHMIAS

    1. ADENOSINE:

    Actions: it has a variety of roles including energy transfer, promotion ofprostaglandin release, inhibition of platelet aggregation, antiadrenergic effectscoronary artery dilatation & suppression of heart rate

    Uses: strong depressant of SA & AV node. Used in paroxysmal supraventricular

    tachycardia

    Side effects: flushing, dyspnea, chest pressure, nausea, head ache

    Adverse effects: Are short lived because the half life of adenosine is only 10

    seconds

    Drug interactions: Enhanced effect with- dipyridamole & carbamazipines

    2. AMIODARONE:

    Actions: action is unknown. This is a class III agent that acts by prolonging theaction potential of atrial and ventricular tissues and by increasing the refractory

    period w/o altering the RMP, thus delaying repolarization

    Uses: SVT, atrial fibrillation & flutter, bradycardia-tachycardia syndrome, &hypertrophic cardiomyopathies

    Side effects: chest pain, fatigue, syncope, palpitations, edema

    Adverse effects: narrowing of pulse pressure, dyspnea, ataxia, confusion, bluuredvision, yellow brown pigments in the cornea, photosensitivity & liver damage

    3. BETA ADRENERGIC BLOCKING AGENTS:

    Actions: Class II agents. They block the cardiac response to sympathetic nervestimulation by blocking the beta receptors, as a result, the HR, BP & CO reduces

    Uses: sinus tachycardia, paroxysmal atrial tachycardia, PVC

    4. BRETYLIUM

    Actions: inhibits the release of norepinephrine. This is a class III agent

    Uses: ventricular arrhythmias

    Side effects: dizziness, n/v

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    Adverse effects: hyper/hypotension

    Drug interactions: digitalis glycosides

    5. DISOPYRAMIDE:

    Actions: class Ia antiarrhythmic agent

    Uses: for atrial fibrillation, Wolf-Parkinson-White syndrome, ventriculartachycardias

    Side effects: dryness of mouth & throat

    Adverse effect: bradycardia/heart failure, urinary hesitancy, constipation

    6. FLECAINIDE:

    Actions: Class Ic antiarrhythmic agent. This agent has a negative inotropic effectthat can lead to worsening of heart failure.

    Uses: ventricular tachycardias, PVCs.

    Side effects: dizziness, syncope, blurred vision, headache, n/v

    Adverse effects: edema, increasing dyspnea, arrhythmias

    Drug interactions: agents that enhance its effect: amiodarone, cimetidine,

    disopyramide

    7. LIDOCAINE:

    Actions: Class Ib agent

    Uses: most commonly used drug for ventricular arrhythmias & the drug of choice

    for ventricular arrhythmias secondary to AMI

    Side effects: muscle twitching, light-headedness

    Adverse reactions: respiratory depression

    Drug interactions: Enhanced effect with- phenytoin, procainamide, tocainide, beta

    blockers

    8. MEXILETINE:

    Actions: Class Ib anti-arrhythmic agent similar to lidocaine

    Uses: PVCs, ventricular tachycardias

    Side effects: n/v, dyspepsia

    Adverse effects: neurotoxic, arrhythmia

    Drug interaction: reduced effect with phenytoin

    9. MORICIZINE:

    Actions: inhibits the influx of sodium ions into the myocardial cells, making it a

    class I agent

    Uses: ventricular arrhythmias

    Side effects: dizziness, hypotension, nausea

    Adverse effects: arrhythmias, euphoria

    Drug interactions: enhanced effect with digoxin, cimetidine, & propranolol

    10. PHENYTOIN:

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    Actions: Class Ib drug

    Uses: paroxysmal atrial tachycardia, ventricular arrhythmias

    Side effects: n/v, sedation, drowsiness, blurred vsion

    Adverse effect: Confusion, dermatologic manifestations

    Drug interactions: enhanced effect with- warfarin, disulfiram, INH,

    carbamazipine, chloramphenicol, amiodarone, sulfonamides

    11. PROCAINAMIDE:

    Actions: Class Ia drug that has many cardiac effects similar to quinidine

    Uses: ventricular & supraventricular arrhythmias

    Side effects: drowsiness sedation, dizziness

    Adverse effects: myalgia, arthralgias, skin eruptions

    Drug interactions: Enhanced effect with- histamine receptor blockers, quinidine,

    trimethoprim & beta blockers

    12. PROFAPENONE:

    Actions: Class Ic agent, that has a weak beta blocking & calcium channel

    blocking effect

    Uses: Paroxysmal atrial fibrillation, & ventricular tachycardia

    Side effects: n/v, dizziness, constipation

    Adverse effects: arrhythmias

    Drug interactions: Enhanced effect with quinidine & cimetidine

    13. QUINIDINE:

    Actions: derived from the cinchona bark. It is a class Ia agent. It slows down the

    heart rate & changes a rapid, irregular pulse to a slow regular pulse

    Uses: atrial fibrillation, atrial flutter, PSVT, PVC Side effects: diarrhea, dizziness

    Adverse effects: Cinchonism- fever, chills, tinnitus

    Drug interactions: enhanced effect with- cimetidine, procainamide, digitalis,

    phenothiazines, verapamil, beta blockers

    14. TOCAINIDE:

    Actions: Class Ib agent. This is the first available derivative of lidocaine

    Uses: ventricular tachycardia

    Side effects: n/v, dizziness, cofusion, numbness

    Adverse effects: dyspnea, wheezing, thrombocytopenia

    Drug interactions: enhanced effect with- procainamide, disopyramide, quinidine

    E. DRUGS USED FOR ANGINA PECTORIS

    1. NITRATES:

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    Actions: oldest effective therapy for angina pectoris. They relieve angina by

    inducing relaxation of peripheral vascular smooth muscles, resulting in dilatationof arteries & veins, this reduces venous blood return to the heart leading to a

    decreased oxygen demand in the heart. Nitrates also increase myocardial oxygen

    supply by dilating large coronary arteries & redistributing blood flow, enhancing

    oxygen supply to ischemic areas Uses: Ntroglycerine- DOC for angina pectoris

    Side effects: headache, tolerance

    Adverse effects: excessive hypotension

    Drug interactions: alcohol, calcium ion antagonist, beta blockers

    Agents: amyl nitarite, ISDN, ISMN, nitroglycerine2. BETA BLOCKERS:

    Actions: reduces myocardial oxygen demand by blocking the beta receptors of the

    heart.

    Uses: for angina

    3. CALCIUM ION ANTAGONISTS

    Actions: inhibits the movement of calcium ions across cellular membranes

    Agents: amlodipine, nifedipine, verapamil

    F. DRUGS USED FOR PERIPHERAL VASCULAR DISEASES

    1. PENTOXIFYLLINE

    Actions: hemorrheologic agent. It increases RBC flexibility, decreases the

    concentration of fibrinogen in blood & prevent aggregation of RBc & platelets

    Uses: for intermittent claudication

    Side effects: n/v, dyspepsia, dizziness, HA

    Adverse effects: chest pain arrhythmias, dyspnea

    Drug interactions: Antihypertensive agents, theophylline

    2. CYCLANDELATE:

    Actions: Vasodilator. Directly relaxes smooth muscles in blood vessels

    Uses: intermittent claudication, thromboangitis obliterans, leg cramps, Reynauds

    disease

    Side effects: flushing, tingling, n/v Adverse effects: diaphoresis

    Drug interactions: no known drug interactions

    3. ISOXSUPRINE HCL

    Actions: vasodilator.

    Uses: Buergers disease, Reynauds disease, arterial occlusive disease

    Side effects: same as (2)

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    Drug interactions; Antihypertensive agents

    4. PAPAVERINE HCL

    Actions: vasodilator

    Uses: cerebral & peripheral ischemia

    Side effects: same as 2 & 3 Drug interactions: antihypertensive agents

    5. PHENOXYBENZAMINE HCL:

    Action: vasodilator

    Uses: Reynauds disease, leg ulceration, frostbite

    Side effects: nasal stiffiness, tachycardia

    Adverse effects: hypotension

    Drug interactions: antihypertensives

    6. TOLAZALINE:

    Actions: vasodilator

    Uses: Reynauds disease, chronic leg ulcers, frost bite gangrene

    Side effects: flushing, tingling, sweating, n/v

    Adverse effects: arrhythmias, tachycardias, anginal pain, hallucination

    Drug interactions: antihypertensives

    7. CILOSTAZOL

    Actions: Platelet aggregation inhibitor. Inhibits CAMP phosphodiesterase IIIresulting in vasodilatation, & inhibited platelet aggregation

    Uses: Intermittent claudication

    Side effects: dyspepsia, diarrhea, dizziness Adverse effects: chest pain, palpitations, arrhythmias

    Drug interactions: dilatiazem, erythromycin, omeprazole, fluconazole, sertraline,

    ketoconazole, grapefruit juice

    G. DRUGS USED FOR DIURESIS

    1. CARBONIC ANHYDRASE INHIBITORS: ACETAZOLAMIDE

    Actions: a weak diuretic that acts by inhibiting the enzyme, carbonic anhydrase

    w/in the kidneys, brain and eyes. It promotes the excretion of potassium water &

    bicarbonates Uses: for glaucoma patients. Not commonly used

    2. METHYLXANTHINES: AMINOPHYLLINE:

    Actions: acts by improving blood flow to the kidneys

    Uses: rarely used as a diuretic

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    3. LOOP DIURETICS:

    a. BUMETAMIDE:

    Actions: a potent diuretic that acts by inhibiting sodium & chloride reabsortion

    from the ascending loop of Henle in the glomeruli of the kidneys. It also acts by

    increasing renal blood flow into the glomeruli & inhibits electrolyte absorption in

    the proximal tubule, enhancing Na, chloride, PO3, HCO3 excretion in the urine.Diuretic activity starts 30-60 minutes after administration

    Uses: CHF, renal & liver disease, including nephritic syndrome

    Side effects: gastric irritation, hives

    Adverse effects: hypokalemia, changes in mental status

    Drug interactions: alcohol, barbiturates, digitalis, aminoglycosides, cisplastin,

    NSAIDS, steroids

    b. ETHACRYNIC ACID:

    Actions: acts on the ascending limb of the loop of Henle to prevent sodium and

    chloride reabsorption. Its effect starts 30min, peaks after 2 hours and lasts for 6-8hours.

    Uses: renal & liver diseases, CHF

    Side effects: orthostatic hypotension

    Adverse effects: Hypokalemia, change in mental status, deafness, GIT bleeding,hyperglycemia

    Drug interactions: aminoglycosides, cisplastin, NSAIDS, difitalis, steroids

    c. FUROSEMIDE:

    Actions: acts on the ascending loop of Henle but also affects the proximal & distal

    tubules to prevent sodium & chloride reabsorption. Effect starts 5-10 minutes

    after IV administration peaks after 30 minutes and lasts for 2 hours

    Uses: liver & renal diseases, CHF, HTN

    Side effects: oral irritation, hypotension

    Adverse effects: Electrolyte imbalance, dehydration, hyperuricemia,hyperglycemia

    Drug interactions: Digitalis, propranolol, aminoglycosides, cisplastin, NSAIDS,

    salicylates, phenytoin

    d. TORSEMIDE

    Actions: sulfonamide type loop diuretic

    4. THIAZIDES:

    Actions: Benzothiadiazides acts primarily on the distal tubules of the kidneys to

    block the reabsorption of sodium & chloride ions.

    Uses: CHF, renal & liver disease, obesity, premenstrual syndrome

    Side effects: hypotension, n/v, constipation, gastric irritation

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    Adverse effects: Electrolyte imbalance, hyperuricemia, hyperglycemia

    Drug interactions: digitalis, steroids, lithium, NSAIDS, oral hypoglycemic agents

    5. POTASSIUM SPARING DIURETICS:a. AMILORIDE:

    Actions: exact mechanism of action is unknown, but it acts on the distal renal

    tubule to retain K & excrete Na resulting in a mild diuresis

    Uses: combined with other diuretics. For CHF

    Side effects: n/v, anorexia, headache, flatulence

    Adverse effects: electrolyte imbalance (HyperK)

    Drug interactions: Lithium, K supplements

    b. SPIRONOLACTONE:

    Actions: blocks the sodium retaining & potassium & magnesium excretingproperties of aldosterone, resulting in loss of water with increased sodium

    excretion

    Uses: used in relieving edema & ascites. It also shows reduction in morbidity &

    mortality in a CHF patient

    Side effects: diarrhea, headache

    Adverse effects: mental confusion, electrolyte imbalance, gynecomastia, reduced

    libido, breast tenderness

    Drug interactions: K supplements, salt substitute

    c. TRIAMTERENE:

    Actions: blocks the exchange of potassium for sodium in the distal tubule of thekidneys, resulting in K retention & Na excretion

    Uses; Combined with thiazides

    Side effects: leg cramps, nausea,

    Adverse effects: electrolyte imbalance, dehydration

    Drug interactions: DO NOT ADMINISTER WITH POTASSIUM

    SUPPLEMENTS= HYPERKALEMIA

    6. COMBINATION DIURETIC PRODUCTS:

    Spironolactone + HCTZ

    Triamterene + HCTZ AMILORIDE + HCTZ

    H. DRUGS USED TO TREAT THROMBOEMBOLIC DISORDERS

    1. PLATELET INHIBITORS

    a. ASPIRIN

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    Actions: Inhibits thromboxane A2 Uses: TIA

    Side effects: see midterm lecture notes

    b. CLOPIDOGREL:

    Actions: chemically related to ticlodipine. The metabolite of this drug acts toinhibit platelet aggregation. Antiplatelet activity is seen after 3- 7 days

    Uses: TIA, Post MI, Angina pectoris, peripheral arterial disease, stroke

    Adverse effects: Neutropenia, agranulocytosis, GIT blleding

    Drug interactions: phenytoin, tamoxifen, warfarin, torsemide, fluvastatin,

    NSAIDS

    c. DIPYRIDAMOLE

    Actions: inhibits Thromboxane A2, increases CAMP in platelets, potentiating

    prostacyclin-mediated inhibition

    Uses: TIA, thromboembolism

    Side effects: dizziness, GIT distress

    Adverse effects: postural hypotension

    2. ANTICOAGULANTS:

    a. ARDEPARIN

    Actions: this is a LMWH that enhances antithrombin activity against factor Xa

    and thrombin which prevents completion of the coagulation cascade. (Ardeparin).

    DO NOT INJECT IM

    Uses: DVT

    Adverse effects: Bleeding

    b. DALTEPARIN:

    Action: same as ardeparin

    Use: DVT

    Adverse effect: bleeding

    d. ENOXAPARIN:

    Actions: same as a and b

    Uses: DVT, unstable angina

    Adverse effect: bleeding

    e. HEPARIN:

    Actions: acts as catalyst to accelerate the rate of action of a naturally occurringinhibitor of thrombin, antithrombin III (heparin cofactor).

    Uses: cerebral embolism, DVT, PE

    Side effects: BLEEDING

    Antidote is protamine

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    f. WARFARIN:

    Actions: inhibits activity of vitamin K ( Factors II, VII, IX ,X)

    Uses: DVT, atrial fibrillation with embolism, PE

    Adverse effect: Bleeding

    Antidote: Vit K

    3. FIBRINOLYTIC AGENTS:

    Actions: activates the conversion of plasminogen to plasmin/ fibrinolysin, w/c

    digests fibrin, dissolving the clot

    Uses: Stroke, MI

    Agents: streptokinase, urokinase, Anistreplase/APSAC, alteplase, reteplase

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