Download Anti Hypertensive

Anti Hypertensive
Anti Hypertensive
Types of HTN:
1.
2.
3.
4.
5.
6.
Alternate HTN.
Mild HTN (DBP 91 -104 MMHg).
Moderate HTN (DBP 105 -114 MMHg).
Severe HTN (DBP < 115 MMHg without End
organ damage).
Malignant HTN (DBP < 115 MMHg with end
organ damage).
Systolic HTN (syst BP <160 MMHg(
ANTI HYPERTENSIVE THERAPY
Diuretics:- 4 major groups
1.
Carbonic anhydrase inhibitors (prox. Tubules)
2. Loop Diuretics



Bumetanide (Bumex)
Ethacrynic acid (Edecrin)
Furosemide (Lasix)
Dose
0.5 – 5 mg
25 – 100 mg
40 – 480 mg
3. Thiazides
and Related Sulfonamide Comp.

Chlorothiazide (Diuril)
125 – 500 mg

Cyclothiazide (Anhydron)
0.5 – 2mg

Hydrochlorothiazide (Esidrix)
12.5 – 50 mg

Polythiazide (Renese)
1 – 4 mg

Methylclothiazide (Enduron)
2.5 – 5 mg

Bendroflumethiazide (Naturetin)
2.5 – 5 mg

Benzthiazide (Aquatag)
12.5 – 50 mg

Triclormethiazide (Metahydrin)
1 – 4 mg
Sulfonamide Compounds




Chlorthalidone (Hygroton)
Indapamide (Lozol)
Metolazone (Zaroxolyn)
Quinethazone (Hydromox)
12.5 -50 mls
2 – 5 mg
1 - 10 mg
25 – 100 mg
4. Potassium – Sparing Agents



Spironolactone (Aldactone)
Amiloride (Midamor)
Triamterene (Dyrenium)
25 – 100 mg
5 – 10 mg
50 – 100 mg
MECHANISMS BY WHICH CHRONIC DIURETIC THERAPY MAY
LEAD TO VARIOUS COMPLICATIONS
Diuretic therapy
Renal reabsorption of Na (and Mg)
Hyponatremia
Hypomagnesemia
Saluresis and dluresis
Plasma volume
Cardiac output
Renal blood flow
Postural hypotension
PRA
GFR
Pre-renal
azotemia
Aldosterone
Proximal
reabsorption
uric acid
Hyperuricemia
Distal Ca++
reabsorption
calcium
Hypercalcemia
Kaliuresis
Hypokalemia
Glucose tolerance
Hyper –
cholesterolemia
Dosage and Choice of Agent
Mild & Moderate HTN:
•
•
With serum creatinine > 2 mg/dL
With serum creatinine < 2 mg/dL
Side Effects
1.
Hypolemia

Use small dose of diuretics.
Use moderately long acting (12–18 hours).
Restrict Na+ intake.
Increase dietary K+ intake.
Restrict use of laxative.
Combined Thiazide with K+ sparing agent.





Side Effects (cont.)
2. Hyponatremia
3. Hypomagnesemia
4. Hyperuricemia
5. Hypercholesterolemia
6. Hypercalcemia
7. Hyperglycemia
8. Impotence
9. Use of NSAIDs
Adrenergic Inhibitors:

Peripheral Inhibitors:


Reserphine
Guanethidine (Ismelin)
Guanadrel (Hylorel)
Bethanidine (Tenathan)

Central Inhibitors:

Methyldopa (Aldomet)
Clonidine (Catapres)



* A- Receptor Blockers:
A.
a1- Receptor
Doxazosin ( Cardura)
 Prazosin (Minipress)
B. a1 and a2- Receptors
 Phentolamine (Regitine)
 Phenoxybenzamine (Dibenzyline)

* B- Receptor Blockers
 Acebutolol
 Atenolol
 Betaxolol
 Metoprolol
 Nadolol
 Penbutolol
 Pindolol
 Propranolol
(Sectral)
(Ternomin)
(Kerlone)
(Lopressor)
(Corgard)
(Levatol)
(Visken)
(Inderal)
Beta-adrenoceptor blocking drugs
Nonselective
ISA
+
ISA
Nadolol
Pindolol
Propranolol Carteolol
Timolol
Penbutolol
Sotalol
Alprenolol
Tertalolol
Oxprenolol
Dilevalol
selective
ISA
with alpha-blocking
activity
+
ISA
Atenolol
Acebutolol
Esmolol
(Practolol)
Metoprolol Celiprolol
Bevantolol
Bisoprolol
Betaxolol
Labetalol
Bucindolol
Carvedilol
VASODILATORS
Direct

:
Hydralazine
 Minoxidil
 Nitroproside
 Diazoxide
 Nitroglycerin
 Calcium Blockers
 Converting Enz. Inh.
 Alpha Blockers
A<V
A<V
A<v
A<V
V<A
A<V
A<V
A=V
Pharmacological Effects of Ca+ Blockers
Deltiazem
Verapamil
Nefidipine
Nicardipine
-
-
Heart rate
Myocardial
Contractility
-
-
Nodal
Conduction
-
-
Peripheral
Vasodilation
ACE INHIBITORS


Captopril
Enalipril
 Lisinopril
 Fosinopril
 Ramipril
 Quinapril
 Benazepril
ANGIOTENSION II ANTAGONIST


losartan
Olmesartan
DRUGS COMMONLY USED
B-Blockers
In-patient with angina pectoris
Or Ca + Channel Blockers + Peripheral Vascular Disease
ACE Inhibitor
Or Ca + Blocker
In-patient with DM
++ In patient with hyperlipidemia
Diuretics
Or ACE Inhibitors
In CHF
Diuretics
Or Ca + Blockers
In CRF
Diuretics
Or Ca + Blockers
In Asthma + COPD
TABLE 29-12 PARENTERAL DRUGS FOR TREATMENT OF
HYPERTENSIVE EMERGENCY (IN ORDER OF RAPIDITY OF ACTION)
DRUG
DOSAGE
ONSET OF
ACTION
ADVERSE EFFECTS
VASODILATORS
Nitroprusside
(Nipride,Nitropress)
0.25 -10 ug/kg/min as I.V. infusion
Instantaneous
Nausea, vaomiting,
muscle twitching
sweating, thiocyanate
intoxication
Nitroglycerin
5 -100 ug/min as I.V. Infusion
2 – 5 min
Tachycardia, flushing,
headache, vomiting,
methemoglobinemia
Diazoxide (Hyperstat)
50 – 100 mg/IV bolus, repeated or
15 – 30 mg/min by I.V infusion
2 – 4 min
Nausea, hypotension,
flushing, tachycardia,
chest pain
Hydralazine
(Apresoline)
10 – 20 mg I.V
10 – 50 mg I.M
10 – 20 min
20 – 30 min
Tachycardia, flushing,
headache, vomiting,
aggravation of angina
Enalapril (Vasotec IV)
1.25 – 5 mg q 6 hr
15 min
Precipitous fall in BP
in high renin states;
response variable
Nicardiprine
5 – 15 mg/hr I.V
10 min
Tachycardia,
headache, flushing,
local phlebitis
TABLE 29-12 PARENTERAL DRUGS FOR TREATMENT OF
HYPERTENSIVE EMERGENCY (IN ORDER RAPIDITY OF ACTION)
(Cont.)
DRUG
DOSAGE
ONSET OF
ACTION
ADVERSE EFFECTS
ADRENERGIC INHIBITORS
Phentolamine (Regitine)
5 – 15 mg I.V.
1 – 2 min
Tachycardia,
flushing
Trimethaphan (Arfonad)
0.5 – 5 mg/min as I.V. infusion
1 – 5 min
Paresis of bowel and
bladder, orthostatic
hypotension, blurred
vision, dry mouth
Esmolol ( Brevibloc)
500 ug/kg/min for 4 min, then
150 -300 ug/kg/min I.V.
1 – 2 min
Hypotension
Propranolol (Inderal)
1 – 10 mg load; 3ng/hr
1 – 2 min
Beta blocker side
effects, e.g.,
bronchospasm,
decreased cardiac
output
Laberalol (Normodyne,
Trandate)
20–80 mg I.V. bolus every 10
min
2 mg/min I.V. infusion
5 – 10 min
Vomiting, scalp
tingling, burning in
throat, postural
hypotension,
dizziness, nausea
Table 9 – 35 Adverse Effects of Antihypertensive Agents
Diuretics
Nausea, muscle cramps, hypovolemia, hypokalemia,
hyponatremia, hyperurcemia, hyperglycemia, rash.
Potassium-sparing
diuretics
Hyperkalemia, gynecomastia
Adrenergic inhibitors
Methyldopa
Drowsiness, dry mouth, impotence, hepatitis, postural
hypotension, hemolytic anemia, fever
Reserpine
Somnolence, nasal congestion, nightmares, mental
depression
Gunethidine
Postural hypotension, diarrhea, retrograde ejaculation,
weakness on exertion
Propranolol
Bradycardia, left ventricular failure, asthma, Raynaud’s
syndrome, central nervous system symptoms, sodium
retention
Mecamylamine and
trimethaphan
Postural hypotension, parasympathetic blockade with
constipation and paralytic ileus, loss of visual
accommodation.
Clonidine
Dry mouth, drowsiness, rebound hypertension if drug
stopped abruptly
Table 9 – 35 Adverse Effects of Antihypertensive Agents
(Cont.)
vasodilator agents
Prazosin
Tachycardia, headache, postural weakness and
hypotension
Hydralazine
Lupuslike syndrome, headache, tachycardia, angina
Minoxidil
Tachycardia, hirsutism, headache, sodium retention
Diazoxide
Hyperglycemia, tachycardia, angina, sodium retention
Sodium nitroprusside
Excess hypotension, acute tubular necrosis,
thiocyanate toxicity