Antihypertensive Drugs Flashcards
What are the drugs class we use for HTN?(It’s 10 Dr. Morcos gave)
- Diuretics
- ACEI (Angiotensin converting Enzyme inhibitors
- ARB ( Angiotensin Receptors Blockers
- BB (Beta Blockers
- CCB (Calcium Channels Blockers)
- Alpha 2 agonists
- Adrenergic Neuronal Blocking Drugs
- Alpha Blockers
- Direct acting vasodilators
10.Renin Inhibitors
Which classes of Antihypertensive drugs have proven
To decrease mortality from heart diseases?
A. Beta Blockers
B. ACE inhibitors
C. Thiazides Diuretics
A. Beta Blockers
What is recommended for Elevated Blood pressure?
Life-style modification
Weight reduction
Moderate alcohol intake
Reduction of sodium intake
Smoking cessation
Regular physical activity
What is Stage 1 HTN numbers?
Stage I Hypertension:
Systolic 130-130
Diastolic 80-89
What is recommended. For Stage 1 HTN
Consider one drug: Diuretic, ACEI,ARB or. Ccb
What is the B/P for Stage II HTN? And what is recommended?
Systolic >140
Diastolic >90
2 Drugs combination: Diuretic + ACEI or ARB or CCB
Jan Doe come sin with HTN + Angina Pectoris. What will be the clinical treatment?
Hypertension + Angina Pectoris
Rx: BB and/or CCB
John Doe comes in with HTN + BPH. What will be the clinical treatment?
: Alpha blocker
Jan Wilson comes in with HTN + DM? What will be your treatment plan?
Rx: ACEI or ARB
Luke Walker comes in with HTN + HF what will you prescribe him?
ACEI, ARB, BB, Diuretic,
Judy comes in with HTN + MI. What will be your treatment plan?
BB, ACEI
Billy bob comes in with HTN + Dyslipidemia. What will be your treatment plan?
Alpha blocker, CCB
Drug of choice for Hypertension with diabetes
- BB
- ACEI
- CCB
- Diuretic
In a study of a patient with refractory hypertension, which of the
following antihypertensive combinations will reduce the systolic
BP the most?
A. Adding an alpha blocker to a beta blocker
B. Adding an ARB to an ACEI
C. Adding K+ sparing diuretic to a thiazide diuretic
D. Adding a dihydropyridine CCB to a non-hydropyridine CCB
C
Which of the following activities can have the greatest
effect on blood pressure reading?
A. The consumption of three alcoholic drinks 12 h before the
measurement
B. The drinking of a cup of coffee 1h before the measurement
C. The smoking of a cigarette 15 minutes before the measurement
D. The use of a cuff that is one size too small for the patient.
C
Pregnant female with Pre-eclampsia.
Drug of choice for Hypertension during pregnancy:
Labetalol - Hydralazine – Nifedipine - Nitroglycerin
Mechanism Affecting Blood Pressure
BP = CO x TPR CO = SV x HR
BP = SV x HR x TPR
Mechanism Affecting Blood Pressure
- Increase SV: Edema, increase renin-angiotensin activity
Rx: Diuretics, ACEI or ARB - Increase in HR: Due to decrease vagal tone and increase
Sympathetic tone
Rx: BB - Increase Peripheral resistance: Increase sympathetic tone
Rx: Alpha 2 agonist, alpha blocker, CCB or direct acting
Types of Diuretics
- Thiazide Diuretics
- Loop Diuretics
- Osmotic Diuretics
- Carbonic Anhydrase inhibitors
- K+ sparing Diuretics
Thiazides Diuretics (names)
Mechanism of Action:
Adverse Effects:
Chlorothiazide
Hydrochlorothiazide
Chlorthalidone
Indapamide
Metolazone
Mechanism of Action: Inhibit Na/Cl cotransport
Increase excretion: Na+, K+, Cl-, Mg++, HCO3
Decrease excretion: Ca++, Uric acid
Adverse Effects:
Hyponatremia, Hypokalemia, hypomagnesia, metabolic
alkalosis,
Hypercalcemia and hyperuricemia
Thiazide diuretics increase plasma cholesterol and TGs (except indapamide)
Loop Diuretics(names)
Mechanism of action
Adverse effects:
Furosemide
Bumetanide
Torsemide
Ethacrynic acid
Inhibit the Na+/K+ dichloride cotransport
system
Increase excretion: Na+, K+, Mg++, Cl-, HCO3, and Ca++
Adverse effects: Hyponatremia, hypokalemia, hypomagnesia
Metabolic alkalosis, hypocalcemia and Ototoxicity
Drug Interaction:
Loop diuretic + Antibiotic (aminoglycosides)
Increase risk for Ototoxicity
Osmotic Diuretics(names)
MOA
Side effects
Mannitol
Glycerol
Mechanism of action: Increase the osmotic pressure in the
proximal tubule which
Lead to inhibition of reabsorption of water and electrolytes
Indications:
Increase intracranial pressure (cerebral edema)
Increase intraocular pressure (acute glaucoma)
Acute renal failure
Adverse Effects:
Excessive plasma volume expansion which can lead to heart failure
Carbonic Anhydrase inhibitors
Mechanism of action
Indications
Adverse effects
Acetazolamide
Dorzolamide
Mechanism of action: Increase excretion of Na+, K+, and
HCO3
Indications:
High altitude sickness
Glaucoma
Overdose of acidic drugs (Alkalinize the urine)
Adverse effects
Drowsiness
Paresthesia
K+ Sparing Diuretics(names)
MOA
Side Effects
Indications
Spironolactone (aldosterone antagonist)
Eplerenone (new) less gynecomastia
Amiloride
Triamterene
Mechanism of action: Block Na+ reabsorption
Indications:
Spironolactone +ACEI increased survival in heart failure
Spironolactone is used in Rx of Hirsutism due to its antiandrogenic
effect
Amiloride is used in Rx of Nephrogenic Diabetes insipidus caused by
lithium
Adverse effects:
Hyperkalemia
Nephrolithiasis (Triamterene)
Decrease libido and gynecomastia (Spironolatone)
Treatment of Hyperkalemia: Patiromer
Antidiuretic Hormones Antagonists
Vasopressin Antagonists
MOA
S/E
Indications
Antidiuretic Hormones Antagonists
Vasopressin Antagonists
Conivaptan
Tolvaptan
Mechanism of action:
Conivaptan (V1A and V2 receptors blocker)
Tolvaptan (Selective V2 receptors blocker
Indications:
Euvolemic and hypervolemic hyponatremia
Adverse effects:
Infusion site reaction
Hypokalemia
ACE inhibitors
Angiotensin Converting Enzyme Inhibitors(names)
Widely used drugs ending in “PRIL”
Captopril
Enalapril
Lisinopril
Ramipril
Fosinopril
Benazepril
Quinapril
ACE inhibitors
Angiotensin Converting Enzyme Inhibitors
MOA
- Prevent the conversion of angiotensin I to Angiotensin II
Decrease the vasoconstrictive effects of angiotensin II
peripherally (reduce afterload) and in the kidney causing
efferent arteriolar dilation - Decrease the release of aldosterone which lead to
decrease salt and water retention - Prevent the conversion of Bradykinin to inactive compound
Increase Bradykinin has a good vasodilatory effects
May contributes to dry cough in some patients
ACEI clinical use
S/E
Clinical Use:
Heart failure
LV systolic dysfunction (Post MI)
Hypertension and Diabetes
Stroke
Adverse effects
Hyperkalemia
Angioedema
Proteinuria
Elevated BUN and Cr
ACEI are the drug of choice for patients with Hypertension
and Diabetes
Why?
Diabetic patient tend to develop Nephropathy
ACEI slow down renal damage
Contraindications of ACEI
Contraindications of ACEI
1. Pregnancy may cause Fetopathy
Oligohydramnios, IUGR, Hypocalvaria and renal failure
2. Angioedema
3. Bilateral renal artery stenosis
ARB (Angiotensin II Receptors Blockers) names
Drugs ending in “SARTAN”
Losartan
Valsartan
Candesartan
Irbesartan
ARBs MOA & S/E
Mechanism of action
They block angiotensin II receptors
NO effect on Bradykinin metabolism (no dry cough)
Adverse Effects
Hyperkalemia
Angioedema
Contraindicated in Pregnancy
BB Beta Blockers names
Drugs ending in “OLOL”
Non-Selective B Blockers Propranolol Nadolol Timolol
Selective B1 blockers Metoprolol Atenolol Bisoprolol Betaxolol
B-Adrenergic Partial agonist Acebutolol
B-Blocker and NO release Nebivolol
Non-selective Beta and
alpha Blockers
Carvedilol Labetalol
Clincial use of BB Beta block & S/E?
Clinical use:
1. Coronary artery diseases
2. Tachyarrhythmias
3. Migraine Headaches
4. Anxiety
Adverse effects
Bradycardia
Fatigue
Sexual disfunction
AV Block
Abrupt withdrawal can cause rebound hypertension due
To upregulation of # of receptors
Mask signs of Hypoglycemia
Cautions: Asthma and Heart block
CCB Calcium Channel Blockers names
Drugs ending in “DIPINE”
Dihydropyridines (Vascular Tissues)
Amlodipine
Nifedipine
Felodipine
Isradipine
Nicardipine
Clevidipine
Non-hydropyridines (heart)
Diltiazem
Verapamil
Dihydropyridines
Mechanism of action:
Dihydropyridines
Mechanism of action:
Block L-type Ca++ channels
Causing vasodilation and decrease peripheral resistance
Dihydropyridines
Adverse Effects
Adverse Effects:
Reflex tachycardia
Ankle edema
Gingival hyperplasia
Non-Dihydropyridines:
Mechanism of action * Adverse effects
Non-Dihydropyridines:
Mechanism of action
Decrease heart rate and conduction velocity
Adverse effects
AV conduction block
Constipation
What are the Alpha 2 agonists use for HTN
Clonidine:
Activates presynaptic alpha 2 receptors
Used in Mild to moderate hypertension
Adverse effects: Edema, rebound hypertension after withdrawal
Alpha Methyl Dopa:
Prodrug
Safe in pregnancy
Agonist at the presynaptic alpha 2 receptors
Adverse Effects: Autoimmune hemolytic anemia
(+ve Coombs test)
Hepatitis
Adrenergic Neuronal blocking agents
Guanethidine
Binds to storage vesicles and inhibits release of NE
Contraindicated with Tricyclic antidepressants
Reserpine
Binds to storage vesicles and destroys them
It causes depletion of NE, DA, and serotonin
Adverse effects
Major depression
Suicidal thoughts
GI complications
Alpha Blockers(names)
Clinical use
A/E
Prazocin, Doxazocin and Terazocin
Selective antagonists of peripheral alpha 1 receptors
Reduce blood pressure by relaxing vascular smooth muscle
and decrease arteriolar resistance
They are used for Hypertension patients with BPH
Adverse effects
First dose syncope: Orthostatic hypotension
Incontinence in women: When coughing, sneezing or trying
to lift a weight. This is due to alpha blockade relaxing effect
on the bladder.
Retrograde ejaculation
Direct acting Vasodilators(names)
MOA
S/E
Have no effects on ANS
Hydralazine:
Selective arteriolar dilation
Prodrug of NO
Used for moderate to severe hypertension
Adverse effects: SLE like syndrome in “slow acetylators”
Reflex tachycardia
Sodium Nitroprusside
Causes venous and arterial vasodilation through cGMP
Given IV for hypertensive crisis
Adverse effects:
Cyanide poisoning
Controlled by administering sodium nitrite followed by Na
thiosulfate or Vit B12 cyanocobalamin
Direct acting Vasodilators (names part 2)
MOA
S/E
Minoxidil
Potent direct vasodilator
Activates ATP-Dependent K+ channels
Side Effects
Hypertrichosis
Reflex tachycardia and edema
Used as topical hair products for male and female baldness
(Rogaine)
Fenoldopam:
Stimulates D1 and alpha-2 adrenergic receptors
Protects the kidney
What potent VD side effects is Hypertrichosis
Minoxidil
What are the S/E for Hydralazine?
SLE
What VD causes cyanide poisoning
Sodium Nitroprusside
Renin Inhibitor(name)
MOA
S/E
Contraindicated
Renin Inhibitor
Aliskiren
It directly inhibits the enzyme renin
Block the conversion of Angiotensinogen to angiotensin I
Adverse effects
Hyperkalemia
Angioedema
Contraindicated in Pregnancy
Drugs used in Hypertensive Emergencies
- Calcium channel blockers
Nicardipine
Clevidipine - Beta Blockers
Labetalol
Esmolol - Vasodilator/Nitrates
Fenoldopam
