Antihypertensive drugs

Antihypertensive drugs

Ca2+-channel blockers (CCBs)

Renin inhibitors
ACE inhibitors
AT1-receptor blockers
Sympatholytic: CA, PA
 CCBs
nifedipine (dihydropyridines - DHPs), verapamil and diltiazem Nifedipine
Amlodipine
Isradipine
Indications: Nitrendipine

Hypertension
Chronic renal failure

Side effects:

Reflex tachycardia
Pedal edema (ankle)
Gingiva hyperplasia
 Renin Inhibitors
Effect: Aliskiren
↓ AT-I and AT-II
Does not interfere with ACE-induced catabolism of bradykinin

Side effects:
Hyperkalemia
Hypotension
hyperreninemia

Contraindication:
bilateral renal artery stenosis
pregnancy
 ACEI Captopril
Lisinopril
M.A: ↑ bradykinin
AT I ACE AT II Enalapril
↓aldosterone secretion prodrug Perindopril
Trandolapril

K + supplements and K + -sparing diuretics should not be used during ACEI therapy

Indications: Side effects:

HTN Dry coughing
DM with HTN Altered or reduced taste sensation
PMI Skin rash; angioedema
Hyperkalemia
Renal insufficiency in bilateral renal stenosis
Developmental defects and fetal death
contraindicated during pregnancy
 AT1RB
Competitive Losartan
Candesartan
Effects:
Valsartan
↓BP Telmisartan
Inhib. CHT

Cough ???
 Sympatholytics

PA:
CA:
Methyldopa prodrug
Pregnancy
Guanfacine
Moxonidine
Side effects:
drowsiness, depression, nightmares, dry mouth, nasal stuffiness
 Implications For Dentistry

• NSAIDs
• β-beockers (non-selec.)
• CA and AAX
 Diuretics
Antidiuretics
 Carbonic anhydrase inhibitors (CAIs)
Acetazolamide
CA : eye, RBC, pancreas, CNS, (sulphonamide) Dorzolamide
Brinzolamide
M.A:
↑ luminal PCT H+ → ↓ Na+/H+ transport activity, rapid rise in urinary HCO3- excretion
to ~35% of filtered load

Ind. : S.E :
• ↑ IOP • Hypokalemia
• Acute mountain sickness • Metabolic acidosis (alkaline urine), excretion
• Metabolic alkalosis of weak acids
• Adj.: Epilepsy, edema • Allergic reaction (skin)
Loop Diuretics (INHIBITORS OF NA+-K+-2CL- SYMPORT)
high ceiling or high efficacy diuretics Furosemide
Ethacrynic acid
M.A : Inh. activity of the Na+-K+-2Cl– symporter in the
TAL

Ind. : S.E :
• Cardiac, pulmonary, nephrotic, • Abnormalities of fluid and electrolyte balance
hepatic edema • Hyponatremia
• Chronic CHF • EC fluid volume depletion
• Refractory Hypertension • Hypokalemia
• Hypercalcemia • Hypomagnesemia-Hypocalcemia
• Ototoxicity (Ethacrynic acid)
• Hyperuricemia-hyperglycemia
• Allergy
Thiazide diuretics (INHIBITORS OF NA+-CL- SYMPORT)
Hydrochlorothiazide (HCT)
M.A : Inh. NaCl transport in DCT
Indapamide
 high excretion of filtered Na+  Clopamide
 ↑ K + excr. Chlortalidone
 Acute use, ↑ UA excr. ; chronic use ↓ UA
excr.
 Chronic use → ↑ Mg2+, ↓ Ca2+ excr.
S.E :
Ind. :
• Allergy
• Edema (cardiac, hepatic and renal failure) • EC volume depletion, hypotension,
• Hypertension (alone or in comb.) hypokalemia
• Nephrogenic DI (↓urine volume by up to • Hyponatremia, metabolic alkalosis,
50%) hypomagnesemia, hypercalcemia, and
• prevent the formation of renal stones hyperuricemia.
• Metabolic acidosis
 Osmotic diuretics
p.o : glycerin , isosorbide
i.v : mannitol,
M.A:
 Act in PCT and LH
 ↑ Na+, K+, Ca2+, Mg2+, Cl–, HCO3-  & PO4-3 excr

Ind. : S.E :

• Dialysis • Expand extracellular fluid volume →

• Acute attacks of glaucoma pulmonary edema (patients with heart failure
• Cerebral edema or pulmonary congestion)
• Hyponatremia → headache, nausea, vomiting
• Dehydration
K+-Sparing diuretics (inhibitors of renal epithelial Na+ channels)
Triamterene and amiloride are the only 2 drugs of this class in clinical use.
Aldosterone antagon., K+-sparing diuretics
Spironolactone
Eplerenone
M.A : ↑ Na+ , ↓ (K+ , H+ , Ca2+ and Mg2+ ) excr.

Ind. :
• In combination with LD & Th.D (edema, hypertension)
• Liddle syndrome, Hyperaldosteronism
• Prevent hypokalemia

S.E:

• Sex hormone irregularities

• Hyperkalemia
 Antidiuretic Hormone Antagonists

nonpeptide competitive antagonists V2 Tolvaptan

M.A: aquaporins

↑ urine osmolality ↓ plasma volume ↑ plasma osmolality ↑ Na+ concentration

Ind.:
• hyponatremia (euvolemic and hypervolemic)
• CHF

Side effects:
• thirst, headache, hypokalemia, and vomiting
• vasodilatation and hypotension block of V1A
• hepatotoxicity
Thank you for your attention