antihypertensive drugs antihypertensive drugs lector prof. posokhova k.a

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  • Antihypertensive drugsLector prof. Posokhova K.A.

  • FREQUENCY of arterial hypertension (AH)AP > 140/90 mm Hg

    20-30 % in populationAt elderly people - 45-50 %

  • Principles of treatment of arterial hypertension 1. Treatment should be started as soon as possible and should be hold till the end of life. Canceling antihypertensive drugs administration causes relapse of AH.2. All the individuals with increased arterial pressure should obtain drugless treatment (modifying lifestyle):-rejection from smoking and alcohol;-increasing of physical activity;-restriction of salt consumption (less than 6 g per day);-decreasing of body weight in a case of obesity.3. Scheme of drug treatment should be the most availably simple 1 tablet per day if possible; it is better to use drugs with long duration of action (prophylaxis of considerable fluctuation of blood pressure during the day).4. Rapid decreasing of blood pressure to low figures is dangerous, especially for elderly patients.5. Main aim of the treatment is to decrease blood pressure to 140/90 mm Hg. To improve life prognosis is the aim that has a more significant meaning than character of drugs used to reach this aim. It is better to prescribe cheap and non modern drugs than dont treat the patient at all.

  • Treatment of arterial hypertension

    Drugs of first row-diuretics (furosemid, dichlothiazide, spironolacton) -inhibitors of ACE (captopril, enalapril, ramipril)-antagonists of angiotesine II receptors (R ) (losartan)--adrenoblockers (anaprilin, atenolol, thymolol) --adrenoblockers (prasosine, terasosine)--, -adrenoblockers (labetolol, carvedilol)-Ca ions antagonists (niphedipine, amlodipine, verapamil)Drugs of second row :-agonists of 2 adrenoreceptors of central action (clopheline, methyldopa)-sympatholytics (reserpin, octadin)-direct vasodilators (molsidomin, hydralasin)New drugs:-imidasolines (moxonidine, rilmenidine)-serotonin receptors blockers (ketanserin) -monateril (calcium antagonist, 2 -adrenoblocker)

  • Mechanism of action of thiaside diureticsin case of arterial hypertensionDychlothiaside(hypothiaside)Oxodolin (chlortalidon, hygroton)Thiaside diuretics Holding sodium and water Volume of circulating blood Cardiac output Peripheral vascular resistanceDecreasing of arterial pressure

  • FUROSEMIDE High ceiling (loop) diuretic Properties : 1. diuretic action 2. dilation of peripheral venous 3. decrease left ventricular filling pressure 4. potent anti-inflammatory effect (similar to indometacine and other NSAID) Administration: hypertensive emergencies, long-term treatment of arterial hypertension Adverse reactions: dehydration, hypokalemia, hearing loss - deafness, hypocalcaemia

  • THIAZIDES and RELATED DIURETICSMedium efficacy diureticsBenzothiadiazines (chlorothiazide, hydrochlorothiazide, clopamide), related thiazide like (chlorthalidone, indapamide)for long-term treatment of arterial hypertesion (oral administration)Duration of action (6-12 hours for hydrochlorothiazide, 12-18 hours for clopamide, 48-50 hours for chlorthalidone)Adverse reactions: dehydration, hypokalemia, hyperuricaemia (rise of blood urate level)

  • Furosemid (diuretic)

  • Furosemid (diuretic)

  • Triampur(triamteren + hydrochlorthiaside)diuretic

  • Mechanism of action of beta-adrenoblockers(anaprilin, atenolol, methoprolol etc.)in case of arterial hypertension -adrenoblockers activation of 1-adrenoreceptors of heart Cardiac output Angiotensine Renin Aldosterone Holding sodium and water Peripheral resist- ance of vessels Volume of blood circulationDecreasing of blood pressure

  • -adrenoblockersUsed for mostly mild to moderate cases of AH (frequently in combinations with other drugs)Stable hypotensive response develops over 1-3 weeksTitration the effective doseAntihypertensive action is maintained over 24 hr after single daily doseWithdrawal syndrome if discontinue quickly Contraindications: bronchial asthma, peripheral vascular disease, diabetes

  • Atenolol - adrenoblocker

  • Anaprilin 1- 2 adrenoblocker

  • Vasocardin 100 mgMethoprolol tartrate

  • Nadolol( 1, 2 - adrenoblocker )

  • Tenoretic(atenolol + chlortalidon)

  • 1-adrenergic blockers(prazosin, terazosin, doxazosin)Do not block presynaptic 2-adreno-receptors, so do not cause reflex cardiac stimulation (as compared to nonselective -adrenoblockers)

    Dilate resistance and capacitance vessels

    Adverse effects: postural hypotension (effect of first dose), tolerance gradually develops with monotherapy

  • Prasosine (1 adrenoblocker)

  • , adrenoreceptors blockers(labetalol, carvedilol)Labetalol is used for long-term treatment of AH and for emergencies (i. v. - hypertensive crisis, clonidine withdrawal, cheese reaction)

    Carvedilol produces vasodilatation, antioxidant/free radical scavenging properties, it is used for HD and for CHF

  • MECHANISM OF ACTION OF IACEDecrease of arterial pressuresympathetic tone peripheral vessels tone retention of Na+ and H2O bradicinineANGIOTENSINOGENANGIOTENSIN(inactive)IACEDecrease angiotensine IIproductionDecrease aldosteroneproduction- ACERenin (kidneys)

  • IACE (ANGIOTENSIN CONVERTING ENZYME INHIBITORS)Captopril, enalapril, ramipril, perindopril etc.Decrease the levels of mortality and morbidityWhen used for monotherapy control AP in 50% of patientsFrequently combined with diuretics (not with potassium-sparing diuretics !) and -adrenoblockers - the effectiveness of therapy grows to 90%Adverse effects: cause the retention of potassium ions, dry persistent cough (requires discontinuation of IACE or treatment with NSAID)Contraindicated for the patients with bilateral renal artery stenosis)

  • Captopril (IACE)

  • KOZAAR (Losartan) R

  • CALCIUM CHANNEL BLOCKERS (dihydropyridines DHPs)Short acting DHPs (nifedipine) can increase mortality as a result of reinfarction (long term controlled trials)Retard forms of DHPs (Amlodipine) are used widely for AHDo not contraindicated in asthma, do not impair renal perfusion, do not affect male sexual functionCan be used during pregnancy Can be given to diabeticsAdverse reactions: ankle edema, slight negative inotropic / dromotropic action, nifedipine decreases insulin release (diabetes accentuating)

  • NIFEDIPINE(calcium channels blocker)

  • NIFEDIPINE(calcium channels blocker)

  • NIFEDIPINE(calcium channels blocker)

  • NIFEDIPINE(calcium channels blocker)

  • NORVASC (AMLODIPINE) (calcium channels blocker)

  • recommended drugto use carefullydiseasesDRUGSCalcium channels blockers administration

    Arterial hypertension

    Verapamil

    Dilthiasem

    Niphedipin

    Felodipin

    Amlodipin

    Ischemic heart disease

    Dilthiasem

    Niphedipin

    Amlodipin

    Verapamil

    Supraventriculetachicardia

    Verapamil

    Dilthiasem

    Possibility to combine with beta-blockers

    Dilthiasem

    Niphedipin

    Amlodipin

    Felodipin

  • CLOPHELINE2 - adrenergic receptors agonist (in brainstem stimulates 2 - adrenergic receptors and imidazoline receptors)decreases vasomotor centers tone - reduces sympathetic tone - fall in APIncreases vagal tone - bradycardiaHas analgesic activityFor hypertensive emergencies (i. v. dropply or very slowly)Side effects and complications: postural hypotension, sedation, mental depression, sleep disturbance, dry mouth, constipation, withdrawal syndrome

  • CLOPHELINE(decreases vasomotor centers tone)

  • SINEPRESS(dihydroergotoxine + reserpine + hydrochlorthiaside)

  • TRIRESIDE(reserpine + hydralasine + hydrochlorothiaside)

  • CRISTEPIN(clopamide + dihydroergocristine + reserpine)

  • MANAGEMENT OF HYPERTENSIVE EMERGENCY (intravenously)

    DrugDoseOnsetSide effectsSodiumnitroprussid 0,5-10 mcg/kg/min (dropply)immediatelynausea, vomiting, fibrillation of muscles, sweatingNitroglyceri-num5-10 mcg/kg (dropply)2-5 mintachicardia, flushing, headache, vomiting,Diazoxidum50-100 mg (quickly)300 mg (during 10 min)2-4 minnausea, vomiting,, hypotension, tachicardia, flushing, redness of skin, chest painApressinum10-20 mg10 minflushing, redness of skin, headache, vomitingFurosemidum20-60-100 mg during 10-15 sec2-3 minhypotension, fatigueClophelinum0,5-1 ml 0,01 % solution (in 15-20 ml 0,9 % solution NaCI slowly)15-20 minsomnolenceAnaprilinum5 ml 0,1 % solution (in 20 ml 0,9 % NaCI solution slowly) 20-30 minbradicardiaMagnesiumsulfas5-10-20 ml 25 % solution (i. v. very slowly or dropply)15-20 minredness of skinLabetololum20-80 mg (slowly 10 min) or 2 mg/kg (dropply); the whole dose 50-300 mg5-10 minnausea, vomiting,, hypotension, dizzeness

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