#Antihypertensive drug Written by: Hala Nsour & Huda Etoom

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1 #Antihypertensive drug Written by: Hala Nsour & Huda Etoom

2 Antihypertensive Drugs Average pressure in healthy people is (120/80) but it's ok to raise or reduce a little, to say that this is hypertension patient I must monitor the pressure while he is relax and for a period of time (week) and all result must be higher than normal Hypertension is asymptomatic disease The target of medication to hypertension patients is to minimized the morbidity and mortality Usually hypertension patient has another disease with it, so the physician must take care to individual case Hypertension has two kinds: 1_ essential: unknown causes (90_25%) 2_ secondary: known causes Pressure: is the amount of force applied by blood stream on arteries walls To control hypotension there are two mechanisms: 1_ Sympathetic: *beta1 receptors h increase contractility secretes rennin by kidney *alpha1 receptors increase muscle contraction 2_ Renal system: decrease blood flow to renal so kidney will secrete rennin which convert angiotensin 1 to angiotensin 2 Angiotensin 2 effects: increase peripheral resistance (vasoconstriction)

3 increase cardiac output : h h h so increase the volume of fluid Drugs affect the sympathetic: alpha blockers and beta blockers As we get older our pressure increase Prehypertension patients are people with range less than 140, they almost obese people and with uncontrolled diet... we can treat those people without medications just by proper diet and exercise. to understand (cvs) We must think in it like we think of tap and pipe, the tap is the pump (heart ) if it was open heavily there will be high pressure in the wall of pipes (arteries), and also if we use smaller pipe (constriction to artery ) the pressure will be high, that s why i the treat e t of hyperte sio we must decrease the peripheral resistance or cardiac output if the patient has kidney failure the pressure must be less than 130,because he can't tolerate the high pressure and to elderly the pressure must be less than 150/90 (as we get older our pressure increase) student ask : how i can treat stage 1 hypertension by exercise (with medications ) and we know that the exercise increase the blood pressure?? answer : generally the exercise reduce the lipid in our body, and as we know that the high density of lipid is one of causes of

4 hypertension ( the vascular is narrowest than normal ) and its improve the circulation i think the student mean that the problem is in the elevation of pressure during exercise so the doctor mentioned that the exercises have a wide range from walking to heavy weight exercise and the physician can choose the proper sure all that about out patient who can tolerate the exercise but if it acute case the patient will be in the hospital and there I can control the situation by giving him diuretics and so on The most vulnerable to hypertension are black people (the race affect) مداوم المريض على دوائه Compliance: the compliance is essential in therapy specially in hypertension and the best way to improve it is by make the patient understand the importance of drug and the mechanism of it, also the patient must be aware to the side effects of drug, so he will tolerate and will not stop it. We usually change the drug if it has very strong side effects or if it not useful to patient Slide 7 /min (28:20) If he diabetes it's recommended to start with diuretics

5 When we change the drug we should use one with different mechanism of action (not alternative ) ACE inhibitors and ARBs are alternative, we can't give both of them at the same time First group مدرا : Increased urine output, thus take at morning. Can be enough or may need second agent General mechanism to diuretics is decrease the blood volume thus decrease the pressure Thiazide diuretics may cause hypokalemia, hyperuricemia and, to a lesser extent, hyperglycemia in some patients (unknown reason). Potassium-sparing diuretics prevent the loss of potassium thus i can combine it with the diuretic so i can prevent the hypokalemia If the patient have problems in kidneys I initiate with Loop diuretics. Control Potassium level and prevent the loss of it is very important thing because we need potassium in all pump of our body

6 We have beta 1 and beta 2 receptors, what we care about for heart is beta 1 receptors, thus I prefer selective drug to beta 1 In asthmatic patient must be selective I can't give Propanolol to patient with any respiratory problem Which is stronger activity reduce peripheral resistance or reduce cardiac output? Reduce cardiac output From the adverse effect of beta blockers that it may reduce the high density lipoprotein cholesterol (HDL ) and increasing triglycerides, and this increase the risk of atherosclerosis we should not stop the drug suddenly because the abrupt withdrawal may cause angina, myocardial infarction and some time sudden death to patient with ischemic heart disease, that is why the drug must be stopped gradually, by decrease the dose

7 Slide 20: ACE inhibitors *angiotensin converting enzyme inhibitors *to control the blood pressure we should be sure about the sympathetic system and its receptor and the renin angiotensin- aldosterone system is working normally. If they are working normally the blood pressure will be normal. *ACE inhibitor group end with pril *we prefer this group if the someone have a diabitis, we choose it firstly *problem in the heart we start with b-blockers then ace inhibitor. *its effect in the peripheral vascular resistance not on the cardiac output *ACE inhibitors will not cause reflex effect like b-blocker Slide21,22: * kidney secret renin *liver secret Angiotensinogen *lung and kidney secret ACE *angiotensin is inactive and will not cause any effect *ADH -> anti dicretic hormone ه االي م وق في جسم اانسا اعا ضغط الد لوضعه الط يعي* *groups that work in this mechanism : 1- ACE inhibitor: that prevent the formation of angiotensin 2 2- angiotensin 2 receptor blocker: its form angiotensin 2 but blocks its receptor 3- renin blocker that prevent the formation of angiotensin (this is the newer one) 4- aldosterone secretion antagonist its prevent the secretion of aldosterone that prevent the reabsorbition of fluid, like spironolactone *these groups work in the same system so they are contrandicated with each other because they give the same effect and the same side effect (together they give extra side effect) Slide24: They are equally effective but casely it can differ from patient to patient م ن ال ريض ي سس ع حد اك ر من ال اني ا ليرتا لوحد اك ر من ال اني * *ARBS, ACE-> they save the kidneys from advanced problem in diabetic because it cause vasodilation so it will reduce the overload of blood that infiltrate by the kidney so it save the kidney for longer period Slide 25:

8 Prodrug : سريعا ي ي مفعوله metabolismيدخل الد اء بش ل معين ح يدخل فو ا ال ال د لي ا ي عر لل *the most side effect seen is dry cough angioedema ي ج ع دما ت ع السوائل ت ت ال د قد ت د قد ا ت د )ان فاخا في الشف ت ت العيو (* *we must monitor potassium level *there is a hypertension special in pregnant women and it called gestational hypertension Slide 27: *Newer than ACE, higher cost, equal effectiveness. *This group end by saratan *They don t increase bradykinin levels because they form angiotensin to, ACE inhibitors *will form the bradykinin *The side effect of arbs lower than in ace inhibitors Note: commercially we choose ace inhibitors because they are lower cost than arbs Slide 29: *Renin inhibitors is the most recent drug (its found in 2007) (oriented) كل ما كا الد اء جديد كل ما ي و سعر اع الي الع ل اصعب * *RAAS: renin-angiotensin aldosterone system *shouldn t be combined with ACE or ARB because they work on the same system *the side effect is more less than the previous groups Slide 31: *calcium effectiveness in smooth muscle cell (vessels) end on the contractility of the heart (cardiac muscle) * e give diabetic patient ACE blocker or calcium blocker, if he has heart disease we give him b-blocker *We don t give high dose during short time because there will be tacychardia and the heart may stop working completely (reflex tachychardia) Slide 32: *the chemical classes that they are differ in structure that will lead to diffrent activity *in pharmacology there is something called structure activity relationship اش رها *diphenylalkylamins *dihydropyridines is contraindicated in ARRHYTHIMA صداع : *migrane Note : CCBS -> calcium channels blocker Slide 37:

9 *They are short acting drugs so they require to be as sustained realize shape, *in sustained realize: ي ر الد اء شو شو من ال مع وم : ال الغير مقسوم من ال ف ا تقس ا م ل ا sustained realize ا ي ن قس اانه سيفقد مفعوله *Any drug that cause vasodilation will cause headach Slide 38: * ends by zosin ع د توسيع الوعاء الدمو يقل الضغط فيزيد ن ض الق ب ل عويض ال قص في الضغط في د ع ا حال من ا * reflex hypotension *postural hypotension : when you standing up suddenly after sleeping or setting down you will feel dizzy because of hypotension *a-adreno receptor : have high side effect and low effects Slide 39: *works in the 2 receptors, not selective *labatol the first choice in gestational hyper tension Slide 40: Clonidine ليس ال يا اا ل ه من ال يا ا ل اا ال س ع ي,ا مريض لم يس ب لد اء ا اك ر Slide 42: ست حامل ل ن ع دها ضغط ن و له : methydopa Slide 43: ال وع ااضعف يوجد ع ش ل صيداني احد هو ال ا Minoxidil

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