Brand Name: TELARBI
Generic Name: Telmisartan
Preparations: 20/ 40/ 80 mg Tablets
Pharmacological Category: Angiotensin II receptor blocker

Mechanism of Action (MOA)
TELARBI (Telmisartan) reversibly and selectively binds to angiotensin II AT1 receptor found in vascular smooth muscle and adrenal gland; thereby interfering the binding of angiotensin II to its receptor i.e. angiotensin II AT1 receptor. As angiotensin II is a vasoconstrictor and aldosterone synthesis stimulator, blockage of its effects results in decrease in systemic vascular resistance.

Pharmacokinetics
Absorption: Rapidly from gastrointestinal tract
Onset of Action: 1-2 hours
Bioavailability: Dose dependent (42% after 40 mg dose and 58% after 160 mg dose)
Peak Plasma Concentration: 0.5 to 1 hour
Protein Binding: > 99.5%
Metabolism: Liver
Half-life Elimination: About 24 hours
Excretion: Faeces via bile (>97%), urine (small amount)

Indications and Dosage
• Hypertension: Initially 40 mg once daily; may be titrated to 20 to 80 mg daily depending on response.
• Cardiovascular Risk Reduction: 80 mg daily

Side Effects
• COMMON: Mild and transient including dizziness, headache, dose related orthostatic hypotension
• MAY OCCUR: Hypotension particularly in patients with volume depletion, impaired renal function and rarely rash, urticaria, pruritus, angioedema and raised liver enzyme value.
• REPORTED: Hyperkalaemia, myalgia, and arthralgia; less likely to cause cough than ACE inhibitors; others are respiratory-tract disorders, back pain, gastrointestinal disturbances, fatigue, and neutropenia.
• RARELY REPORTED: Rhabdomyolysis

Contraindications
• Hypersensitivity
• Pregnancy (2nd and 3rd trimesters)-significant risk of fetal or neonatal morbidity and mortality
• Bilateral renal artery stenosis
• With Aliskiren in patients with diabetes

Warnings/ Precautions
• Caution in patients with hepatic impairment or biliary obstruction and renal artery stenosis.
• Volume depletion should be corrected before starting therapy or a low initial dose should be used.
• Since hyperkalaemia may occur, serum potassium concentrations should be monitored, especially in the elderly and patients with renal impairment.
• Potassium sparing diuretics should generally be avoided.

Drug Interactions
• The antihypertensive effects may be potentiated by drugs or other agents that lower blood pressure.
• An additive hyperkalaemic effect is possible with potassium supplements, potassium sparing diuretics or other drugs that can cause hyperkalaemia.
• NSAIDs should be used with caution in patients taking Telmisartan as the risk of renal impairment may be increased particularly in those who are inadequately hydrated; use of NSAIDs may also attenuate the hypotensive effects of Telmisartan.
• Telmisartan may increase serum concentrations of Digoxin.

Pregnancy Category: C in 1st trimester; D in 2nd and 3rd trimester

Presentations
TELARBI 20: 6 X 10’s
TELARBI 40: 10 X 10’s
TELARBI 80: 6 X 10’s