ORAL ANTI-HTN MEDICATIONS

HTN
• SUSTAINED ELEVATION OF BP>140/90

• Normal blood pressure: systolic <120 mmHg

and diastolic <80 mmHg

• Prehypertension: systolic 120 to 139 mmHg or

diastolic 80 to 89 mmHg
 STAGES OF HTN

• Stage 1: systolic 140 to 159 mmHg or diastolic

90 to 99 mmHg

• Stage 2: systolic ≥160 or diastolic ≥100 mmHg

 TREATMENT OPTIONS
• ACE INHIBITORS
• ARBS
• THIAZIDE DIURETICS
• CALCIUM CHANNAL BLOCKERS
• B-BLOCKERS
• ALDACTONE
• LOOP DIURETICS
• VASODILATORS (HYDRALAZINE)
• A2-AGONISTS (METHYLDOPA)
• RENIN INHIBITOTS ( ALISKIREN)
ACE INHIBITORS
ENEALPRIL
RAMIPRIL
CAPTOPRIL
FOSINOPRIL
LISINOPRIL
QUINAPRIL
ACE INHIBITORS how do they work?

Angiotensin II is a very potent chemical produced by the

body that primarily circulates in the blood. It causes the
muscles surrounding blood vessels to contract, thereby
narrowing vessels.

The narrowing of the vessels increases the pressure within the

vessels causing HTN.

Angiotensin II is formed from angiotensin I in the blood by

the enzyme (ACE).

ACE inhibitors inhibit the activity of the enzyme ACE, which

decreases the production of angiotensin II.
 SIDE EFFECTS
• Dry cough
• Abdominal pain
• Diarrhea
• Dizziness
• Fatigue
• Headache
• Loss of appetite
• Nausea and vomiting
• Chest pain
• Fainting
• Numbness or tingling in the hands or feet
• Rash
• Angioedema
• Hyperkalemia specially when combined with NSAIDS or ARBs
• PRENANCY CATEGORY : D
• CONTRAINDICATED DURING LACTATION .
 ENALAPRIL

• DOSING:

The usual oral dose for treating HTN is 5-40

daily in two divided doses.
 RAMIPRIL

• DOSING:

The usual dose of ramipril for HTN is 2.5-20 mg

a day as a single dose or two divided doses.
 CAPTOPRIL

• DOSING:

The recommended dose of captopril for

treating HTN in adults is 25-150 mg two or
three times daily. MAXIMUM DOSE 450 MG/DAY
 BEST TO USE ACEi
• ACE inhibitors are first-line therapy in all
patients who have HF or asymptomatic LV
dysfunction.
• In all patients who have had an ST elevation
MI, or a non-ST elevation MI.
• Diabetes.
• And in patients with proteinuric chronic
kidney disease.
 ARBs
candesartan

eprosartan

irbesartan

Valsartan

losartan

olmesartan
 HOW DO THEY WORK?
Angiotensin II receptor blockers (ARBs) are
medications that block the action of
angiotensin II by preventing angiotensin II
from binding to its receptors on the muscles
surrounding blood vessels.
As a result, blood vessels enlarge (dilate) and
blood pressure is reduced.
• PRENANCY CATEGORY : D
• CONTRAINDICATED DURING LACTATION .
 SIDE EFFECTS
• Abdominal pain
• Diarrhea
• Dizziness
• Fatigue
• Headache
• Loss of appetite
• Nausea and vomiting
• Chest pain
• Fainting
• Numbness or tingling in the hands or feet
• Rash
• Angioedema less than ACE i.
• Hyperkalemia specially when combined with NSAIDS or ACEi.
 VALSARTAN

• DOSING:
INITIAL DOSE 80 MG UP TO 320 MG /DAY
 CANDESARTAN

• DOSING:
INITIAL DOSE 8MG UP TO 32 MG /DAY
 LOSARTAN

• DOSING :
INITIAL DOSE 25 MG UP TO 100 MG /DAY
 BEST TO USE ARBs
• The specific indications for and efficacy of
angiotensin II receptor blockers (ARBs) are
similar to those with ACE inhibitors

• An ARB is particularly indicated in patients

who do not tolerate ACE inhibitors (mostly
because of cough).
THIAZIDES

HCT

METALAZONE

CHLORTHALIDONE
 HOW DO THEY WORK?

• The thiazide diuretics primarily inhibit sodium

transport in the distal tubule.

• They inhibit NaCl by competing for the

chloride site on the transporters.
 SIDE EFFECTS
• Dizziness, fever,
• headache, restlessness.
• vertigo
• Rash
• Hypotension
• Pancytopenia
• Jaundice
• Muscle spasm
• hypokalemia, hyponatremia, hypomagnesemia.
• Impaired glucose tolerance.
• PREGNANCY C
• LACTATION: CAN BE USED
 HCT

• DOSING :
INITIAL DOSE 12.5 MG UP TO 50 MG /DAY
 METALAZONE

• DOSING :
2.5 TO 5 MG /DAY
B-BLOCKERS
ATENOLOL
METOPROLOL
PROPRANOLOL
BISOPROLOL
TIMOLOL
ESMOLOL
LABETALOL
CARVIDOLOL
 HOW DO THEY WORK?

• THEY DECREASE HR AND DECREASE CARDIAC

DEMAND.

• THEY INCREASE CARDIAC CONTRACTILITY.

• CAN CAUSE PERIPHERAL VASODILATATION.

 SIDE EFFECTS

• HEART FAILURE
• HYPOGLYCEMIA
• FATIGUE , DEPRESSION.
• THEY CAN EXACERBATE PVD.
• BRONCHO-CONSTRECTION
• PREGNANCY B-C
• CAN BE USED DURING LACTATION
 CARVIDILOL

• DOSING:
INITIAL DOSE 6.25 MG IN 2 DOSES AND CAN
INCREASE THE DOSE UP TO 50 MG DAILY
 LABETALOL

• DOSING:
INITIAL DOSE 100MG TWICE DAILY
AND UP TO 2400MG IN 2-4 DIVIDED DOSES.
 BISOPROLO

• DOSING:
INITIAL DOSE 2.5 MG ONCE DAILY
AND UP TO 20 MG /DAY.
 ATENOLOL

• DOSING:
25 MG /DAY AND UP TO 100 MG ONCE
DAILY.
 BEST TO USE B-BLOCKERS
• A beta blocker should be given after an acute
myocardial infarction and to stable patients
with heart failure or asymptomatic left
ventricular dysfunction.

• Beta blockers are also given for rate control in

patients with atrial fibrillation, or control of
angina
 HYDRALAZINE
• Hydralazine can cause a drug-induced lupus-
like syndrome including arthralgias, myalgias,
joint swelling, pericarditis/pleuritis, rash, or
fever.
• PREGNANCY C.
• NOT RECOMMENDED DURING LACTATION.
• INITIAL DOSE 10 MG 4 TIMES DAILY AND UP
TO 25 MG *4.
 CCB
NIFIDIPINE

AMLODIPINE

FELODIPIN

DILTIAZEM

VERAPAMIL
 HOW DO THEY WORK?

• Inhibits calcium ion from entering the “slow

channels” of vascular smooth muscle and
myocardium during depolarization, producing
a relaxation of coronary vascular smooth
muscle and coronary vasodilation.

• Increases myocardial oxygen delivery.

 SIDE EFFECTS
• PERIPHERAL EDEMA.
• VERAPAMIL AND DILTIAZEM CAN EXACERBATE
HEART FAILURE. AND THEY CAN INCREASE RISK
OF MI IN HF PTS.
• RASH
• N/V
• DIZZINESS , FATIGUE.
• MUSCLE CRAMPS.
• PALPITATION AND FLUSHING .
• PREGNANCY C
• NOT RECOMMENDED DURING LACTATION.
 NIFIDIPINE

INITIAL DOSE 30 MG /DAY

CAN BE INCREASED UP TO 120MG /DAY

 AMLODIPINE

INITIAL DOSE 2.5 MG /DAY.

AND UP TO 10 MG DAILY.
 BEST TO USE CCB

• Calcium channel blockers may be preferred in

patients with obstructive airways disease.

• the non-dihydropyridine calcium channel

blockers ( verapamil , diltiazem ) can be given
for rate control in patients with atrial
fibrillation or for control of angina.
 ALDACTONE

• K SPARING DIURETIC.
• DOSE: 25-50 MG DAILY
• PREGNANCY C
• NOT RECOMMENDED IN LACTATION .
• BEST USED IN PTS WITH PRIMARY
HYPER-ALDOSTERONISM.
 SIDE EFFECTS
• Ataxia, confusion, drowsiness, fever,
headache, lethargy.
• Amenorrhea, gynecomastia.
• impotence, irregular menses, postmenopausal
bleeding.
• Renal failure, hyperkalemia.
• Agraneulocytosis.
• n/v , abd pain.
 RENIN INHIBITORS
• ALISKIREN
Work by directly inhibiting renin, resulting in
blockade of the conversion of angiotensinogen
to angiotensin I. Angiotensin I suppression
decreases the formation of angiotensin II
causing peripheral vasodilatation.
Initial dose 150 mg /day and up to 300 mg daily.
 SIDE EFFECTS
• HYPOTENSION.
• RASH.
• HYPERKALEMIA.
• RENAL FAILURE.
• DIARRHEA.
• COUGH.
• ANGIOEDEMA.
• SEIZURE.
• CAUTION WHEN USED WITH ACEi OR ARBs AS IT
CAN CAUSE SEVERE HYPERKALEMIA AND CAN
LEAD TO RENAL FAILURE.

• IT CAN EXACERBATE HYPOGLYCEMIA IN DIABETIC

PTS.

• PREGNANCY D.
 METHYLDOPA
• STIMULATES ALPHA-ADRENERGIC RECEPTORS
CENTRALLY LEADING TO PERIPHERAL
VASODILATATION.
• INITIAL DOSE 250 MG TWICE DAILY AND UP
TO 3 GM /DAY IN DIVIDED DOSES.
• PREGNANCY B
• CAN BE USED DURING LACTATION.
 HTN CRISIS
• INTRODUCTION — A hypertensive emergency
is considered to be present when severe
hypertension is associated with acute end-
organ damage. Usually diastolic bp > 120.

• Examples : encephalopathy, subarachnoid or

intracerebral hemorrhage, acute pulmonary
edema, aortic dissection, ARF .
IV DRUG OPTIONS
Nitroprusside
Nitroglycerin
Labetalol
Nicardipine
Clevidipine
Fenoldopam
Enalaprilat
Hydralazine
 NITROPRUSSIDE

• A rapidly acting arteriolar and venous dilator,

given as an intravenous infusion. Initial dose:
0.25 to 0.5 mcg/kg per min; maximum dose: 8
to 10 mcg/kg per min
 SIDE EFFECTS
• Cardiovascular: Bradycardia, ECG changes,
flushing, hypotension (excessive), palpitation,
substernal distress, tachycardia.
• Central nervous system: dizziness, headache,
increased intracranial pressure, restlessness .
• Dermatologic: Rash .
• Endocrine & metabolic: Metabolic acidosis
(secondary to cyanide toxicity),
hypothyroidism.
• Gastrointestinal: Abdominal pain, ileus,
nausea, retching, vomiting.
• Hematologic: Methemoglobinemia, decreased
platelet aggregation.
• Local: Injection site irritation.
• Neuromuscular & skeletal: Hyperreflexia
(secondary to thiocyanate toxicity), muscle
twitching , miosis.
• Use with extreme caution in patients with
elevated intracranial pressure.
• Use with extreme caution in patients with
hepatic impairment.
• Use with extreme caution in patients with
renal impairment; use the lowest end of the
dosage range; due to risk thiocyanate toxicity
closely.
• Pregnancy c

• Half life 2 minutes

• TRY TO AVOID IN PTS WITH HF OR AORTIC

DISSECTION.
 NITROGLYCERIN
• IT ACTS MORE ON THE VEINS MORE THAN
ARTRIES IN COMPARISION TO
NITROPRUSSIDE.

• BETTER TOLERATED IN PTS WITH HF AND IN

ISCHEMIC PTS.
 IV DOSING

• 5 mcg/minute, increase by 5 mcg/minute

every 3-5 minutes to 20 mcg/minute. If no
response at 20 mcg/minute, may increase by
10-20 mcg/minute every 3-5 minutes
(generally accepted maximum dose: 400
mcg/minute)
• Hemodynamic and antianginal tolerance often
develop within 24-48 hours of continuous
nitrate administration.
• Nitrate-free interval is recommended to avoid
tolerance development.
• gradually decrease dose in patients receiving
GTN for prolonged period to avoid withdrawal
reaction.
 SIDE EFFECTS
• Cardiovascular: Flushing, hypotension, orthostatic
hypotension, peripheral edema, syncope,
tachycardia .
• Central nervous system: Headache (common),
dizziness, lightheadedness .
• Gastrointestinal: Nausea, vomiting, xerostomia .
• Neuromuscular & skeletal: Paresthesia,
weakness.
• Respiratory: Dyspnea, pharyngitis, rhinitis.
• PREGNANCY C

• HALF LIFE 1-4 MINUTES

 LABETALOL

• MODE OF ACTION : Beta-Blocker With Alpha-

Blocking Activity.

• CAN BE GIVEN AS STAT OR INFUSION

 DOSING

• Initial: 20 mg I.V. push over 2 minutes; may

administer 40-80 mg at 10-minute intervals.

• IV INFUSION : 2 mg/minute , usual total dose

required: 50-200 mg.
 SIDE EFFECTS

• Cardiovascular: Hypotension ,edema ,

flushing ventricular arrhythmia.
• Central nervous system: Somnolence
headache, vertigo.
• Dermatologic: pruritus , rash.
• Gastrointestinal: Dyspepsia ,vomiting ,
taste disturbance.
• Hepatic: Elevated Transaminases
• Neuromuscular & skeletal: Paresthesia
weakness.
• Ocular: Vision abnormal.
• Renal: BUN elevation.
• Respiratory: Nasal congestion ,dyspnea.
• PREGNANCY C

• HALF LIFE 5.5 HRS

 NICARDIPINE

• ITS A CALCIUM CHANNEL BLOCKER.

• INFUSION: Initially: 5 mg/hour increased by

2.5 mg/hour every 5 minutes to every 15
minutes up to a maximum of 15 mg/hour.
 SIDE EFFECTS

• FLUSHING , EDEMA, PALPITATIONS , PVCS,

VTACH.
• N/V DYSPEPSIA.
• HYPOKALEMIA , POLYURIA
• INJECTION SITE PAIN AND REACTION.
• WEAKNESS , MYALGIA , PARASTHESIA.
• PREGNANCY C

• HALF LIFE 2-4 HRS

 HYDRALAZINE
• ITS A VASODILATER.

• DOSE: INITIALLY 10 -20 MG IV EVERY 4 HRS

CAN BE INCREASED UP TO 40 MG
EVERY 4 HRS.

IN PRE-ECLAMPSIA GIVE IV 5 MG /DOSE THEN 5-

10 MG EVERY 20-30 MINUTES .
 OTHER DRUGS
• Clevidipine — a calcium channel blocker.
Initial dose: 1 mg/hour; maximum dose: 16
mg/hour.
• Fenoldopam — a peripheral dopamine-1
receptor agonist, given as an intravenous
infusion. Initial dose: 0.1 mcg/kg per min; the
dose is titrated at 15 min intervals depending
upon the blood pressure response
• Enalaprilat — an angiotensin converting
enzyme inhibitor, given as an intravenous
bolus. Dose: 1.25 mg every six hours.

• Propranolol — a ß-adrenergic blocker, given as

an intravenous infusion and then followed by
oral therapy. Dose: 1 to 10 mg load, followed
by 3 mg/h.
 Malignant hypertension and hypertensive
encephalopathy

• A modest reduction of the BP, by no more

than 25 percent of the initial value within the
first 24 hours, with a parenteral vasodilator
usually nitroprusside or labetalol is the initial
strategy for management of malignant
hypertension and hypertensive
encephalopathy.
 Acute pulmonary edema
• Hypertension in patients with acute left
ventricular failure due to systolic dysfunction
should be principally treated with
vasodilators.

• Nitroprusside or nitroglycerin with a loop

diuretic is the regimen of choice for this
problem
Angina pectoris or acute myocardial infarction

• Beta adrenergic blockers should be

administered to all patients without
contraindications who experience a
myocardial infarction.

• Intravenous parenteral vasodilators,

principally nitroprusside and nitroglycerin , are
effective and may reduce mortality in patients
with acute myocardial infarction
 Aortic dissection
• In patients with aortic dissection, an
intravenous beta blocker (labetalol) should be
given to reduce the heart rate below 60 and
maintain the systolic blood pressure between
100 to 120

• Nitroprusside or nitrolycerin can be added to

controle BP.
 Pregnancy

• Intravenous labetalol and hydralazine have

been widely used in pregnant women with
severe hypertension, which is usually due to
preeclampsia or exacerbation of preexistent
hypertension .
 CAUTION

• NEVER STOP ANTI HTN INFUSION ABRUPTLY

AS THIS CAN CAUSE UNOPPOSED A-
ADRENERGIC ACTIVITY THAT CAN CAUSE
SEVERE HTN AND CORONERY ISCHEMIA .
 HYPERTENSIVE URGENCY
• SEVERE ELEVATION OF BP USUALLY >180/120
IN ASYMPTOMATIC PTS. WITH NO END
ORGAN DAMAGE.

• IT OCCURES MORE COMMENLY IN PTS WHO

ARE NON COMPLIANT TO THEIR MEDICATION
OR TO LOW SALT DIET.
• THE GOAL IS TO REDUCE BP TO < 160/100
OVER HRS AND EVEN DAYS

• ALL PTS SHOULD RELAX IN A SILENT ROOM

THIS MEASURE ALONE CAN REDUCE BP BY 10-
20 .
 Previously treated PTS

• Reinstitution of medications in non-adherent

patients.

• Increase the dose of existing antihypertensive

medications, or add another agent.

• Dietary sodium restriction.

 Untreated hypertension
• Initially oral captopril (6.25 or 12.5 mg). Can
be repeated after half to 1 hr .

• the patient is then observed for a few hours,

to ascertain a reduction in blood pressure of
20 to 30 mmHg. Thereafter, a longer acting
agent is prescribed and the patient is sent
home to follow up within a few days.
• USUAL MEDICATIONS ON DISCHARGE ARE
ACEi LIKE ENALAPRIL , CCB LIKE AMLODIPINE
OR NIFIDIPINE , OR THIAZIDES.
THANK YOU