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Product Name
:
MICARDROXI-PLUS
Chemical Name
:
Telmisartan+Hydrochlorothiazide
Therapeutic Category
:
Cardiovascular drugs
Pharmacologic Category
:
Angiotensin II Receptor Blocker - Diuretic, Thiazide
Pharmaceutical Form
:
Tablets
Composition
:
Telmisartan 40mg+Hydrochlorothiazide 12.5mg / Telmisartan 80mg+Hydrochlorothiazide 12.5mg
Monitoring Parameters
Dosing
 
Dosing: Adult
Hypertension: Oral: Replacement therapy: Combination product can be substituted for individual titrated agents. Initiation of combination therapy when monotherapy has failed to achieve desired effects:
Patients currently on telmisartan: Initial dose if blood pressure is not currently controlled on monotherapy of 80 mg telmisartan: Telmisartan 80 mg/hydrochlorothiazide 12.5 mg once daily; may titrate up to telmisartan 160 mg/hydrochlorothiazide 25 mg if needed.
Patients currently on hydrochlorothiazide: Initial dose if blood pressure is not currently controlled on monotherapy of 25 mg once daily: Telmisartan 80 mg/hydrochlorothiazide 12.5 mg once daily or telmisartan 80 mg/hydrochlorothiazide 25 mg once daily; may titrate up to telmisartan 160 mg/hydrochlorothiazide 25 mg if blood pressure remains uncontrolled after 2-4 weeks of therapy. Patients who develop hypokalemia while on hydrochlorothiazide 25 mg may be switched to telmisartan 80 mg/hydrochlorothiazide 12.5 mg.

Dosing: Geriatric

Refer to adult dosing. Monitor renal function.

Dosing: Renal Impairment

Clcr >30 mL/minute: No dosage adjustment necessary.
Clcr ≤30 mL/minute: Not recommended.

Dosing: Hepatic Impairment

Mild-to-moderate hepatic impairment or biliary obstructive disorders: Initial: Telmisartan 40 mg/hydrochlorothiazide 12.5 mg.
Severe hepatic impairment: Not recommended.
Use
 
Treatment of hypertension; combination product should not be used for initial therapy
Adverse Reactions
 
Hypersensitivity to telmisartan, hydrochlorothiazide, sulfonamide-derived drugs, or any component of the formulation; anuria
Contraindications
 
Hypersensitivity to telmisartan, hydrochlorothiazide, sulfonamide-derived drugs, or any component of the formulation; anuria
Warnings / Precautions Drug
 
Boxed warnings:
• Pregnancy: See “Special populations” below.
Concerns related to adverse effects:
• Electrolyte disturbances: Hyperkalemia may occur with angiotensin II receptor antagonists; risk factors include renal dysfunction, diabetes mellitus, and concomitant use of potassium-sparing diuretics, potassium supplements, and/or potassium-containing salts. Use cautiously, if at all, with these agents and monitor potassium closely. Thiazide diuretics may cause hypokalemia, hypochloremic alkalosis, hypomagnesemia, and hyponatremia.
• Ocular effects: Hydrochlorothiazide may cause acute transient myopia and acute angle-closure glaucoma, typically occurring within hours to weeks following initiation; discontinue therapy immediately in patients with acute decreases in visual acuity or ocular pain. Risk factors may include a history of sulfonamide or penicillin allergy.
• Photosensitivity: Photosensitization may occur.
• Renal function deterioration: May be associated with deterioration of renal function and/or increases in serum creatinine, particularly in patients with low renal blood flow (eg, renal artery stenosis, heart failure) whose glomerular filtration rate (GFR) is dependent on efferent arteriolar vasoconstriction by angiotensin II; deterioration of renal function and/or increases in serum creatinine, particularly in patients dependent on renin-angiotensin-aldosterone system; deterioration may result in oliguria, acute renal failure, and progressive azotemia. Small increases in serum creatinine may occur following initiation; consider discontinuation only in patients with progressive and/or significant deterioration in renal function.
• Sulfa allergy: Chemical similarities are present among sulfonamides, sulfonylureas, carbonic anhydrase inhibitors, thiazides, and loop diuretics (except ethacrynic acid). Use in patients with sulfonamide allergy is specifically contraindicated in product labeling, however, a risk of cross-reaction exists in patients with allergy to any of these compounds; avoid use when previous reaction has been severe. Discontinue if signs of hypersensitivity are noted.
Disease-related concerns:
• Aortic/mitral stenosis: Use with caution in patients with significant aortic/mitral stenosis.
• Diabetes: Use hydrochlorothiazide with caution in patients with prediabetes or diabetes mellitus; may see a change in glucose control.
• Gout: In certain patients with a history of gout, a familial predisposition to gout, or chronic renal failure, gout can be precipitated by hydrochlorothiazide.
• Hepatic impairment: Use with caution in patients who have biliary obstructive disorders or hepatic dysfunction; in cirrhosis, avoid electrolyte and acid/base imbalances that might lead to hepatic encephalopathy.
• Hypercalcemia: Thiazide diuretics may decrease renal calcium excretion; consider avoiding use in patients with hypercalcemia.
• Hypercholesterolemia: Use with caution in patients with moderate or high cholesterol concentrations; increased cholesterol and triglyceride levels have been reported with thiazides.
• Hypovolemia: Avoid use or use a smaller dose in patients who are volume depleted; correct depletion first.
• Parathyroid disease: Thiazide diuretics reduce calcium excretion; pathologic changes in the parathyroid glands with hypercalcemia and hypophosphatemia have been observed with prolonged use.
• Renal artery stenosis: Use telmisartan with caution in patients with unstented unilateral/bilateral renal artery stenosis. When unstented bilateral renal artery stenosis is present, use is generally avoided due to the elevated risk of deterioration in renal function unless possible benefits outweigh risks.
• Renal impairment: Use telmisartan with caution with pre-existing renal insufficiency and severe renal impairment. Avoid hydrochlorothiazide in severe renal disease (ineffective); may precipitate azotemia; discontinue or consider withholding if renal impairment occurs.
• Systemic lupus erythematosus (SLE): Hydrochlorothiazide can cause SLE exacerbation or activation.
Concurrent drug therapy issues:
• Angiotensin-converting enzyme (ACE) inhibitors: Concurrent use of ACE inhibitors may increase the risk of clinically-significant adverse events (eg, renal dysfunction, hyperkalemia). Concurrent use with ramipril is not recommended.
Special populations:
• Pregnancy: [U.S. Boxed Warning]: Based on human data, drugs that act on the angiotensin system can cause injury and death to the developing fetus when used in the second and third trimesters. Angiotensin receptor blockers should be discontinued as soon as possible once pregnancy is detected.
Metabolism/Transport Effects
Telmisartan: Inhibits CYP2C19 (weak)
Interactions
 
ACE Inhibitors: Thiazide Diuretics may enhance the hypotensive effect of ACE Inhibitors. Specifically, postural hypotension which can accompany ACE Inhibitor initiation. Thiazide Diuretics may enhance the nephrotoxic effect of ACE Inhibitors. Risk C: Monitor therapy
ACE Inhibitors: Angiotensin II Receptor Blockers may enhance the adverse/toxic effect of ACE Inhibitors. Risk C: Monitor therapy
Alcohol (Ethyl): May enhance the orthostatic hypotensive effect of Thiazide Diuretics. Risk C: Monitor therapy
Antidiabetic Agents: Thiazide Diuretics may diminish the therapeutic effect of Antidiabetic Agents. Risk C: Monitor therapy
Corticosteroids (Orally Inhaled): May enhance the hypokalemic effect of Thiazide Diuretics. Risk C: Monitor therapy
Corticosteroids (Systemic): May enhance the hypokalemic effect of Thiazide Diuretics. Risk C: Monitor therapy
Eplerenone: May enhance the hyperkalemic effect of Angiotensin II Receptor Blockers. Risk C: Monitor therapy
Nonsteroidal Anti-Inflammatory Agents: May diminish the therapeutic effect of Thiazide Diuretics. Risk C: Monitor therapy
Ramipril: Telmisartan may increase the serum concentration of Ramipril. Concentrations of the active metabolite, ramiprilat, may also be increased. Risk C: Monitor therapy
Pregnancy
 
C (1st trimester); D (2nd and 3rd trimesters)
Pregnancy Implications
See individual agents.
Lactation
 
Enters breast milk/not recommended
Breast-Feeding Considerations
It is not known if telmisartan is excreted in human breast milk, use during breast-feeding is not recommended. Thiazides are excreted in human breast milk; benefits to the mother should be weighed against possible risk to the newborn if used in a nursing woman.
Mechanism of Action
 
Telmisartan: Telmisartan is an angiotensin receptor antagonist. Angiotensin II acts as a vasoconstrictor. In addition to causing direct vasoconstriction, angiotensin II also stimulates the release of aldosterone. Once aldosterone is released, sodium as well as water are reabsorbed. The end result is an elevation in blood pressure. Telmisartan binds to the AT1 angiotensin II receptor. This binding prevents angiotensin II from binding to the receptor thereby blocking the vasoconstriction and the aldosterone secreting effects of angiotensin II.
Hydrochlorothiazide: Inhibits sodium reabsorption in the distal tubules causing increased excretion of sodium and water as well as potassium and hydrogen ions
Pharmacodynamics / Kinetics
 
Telmisartan:  Onset of action: 1-2 hours
Duration: Up to 24 hours
Distribution: Vd: 500 L
Protein binding: >99.5%; primarily to albumin and alpha1-acid glycoprotein
Metabolism: Hepatic via conjugation to inactive metabolites; not metabolized via CYP
Bioavailability (dose dependent): 42% to 58%; Hepatic impairment: Approaches 100%
Half-life elimination: Terminal: 24 hours
Time to peak, plasma: 0.5-1 hours
Excretion: Feces (97%)
Clearance: Total body: 800 mL/minute

Hydrochlorothiazide:  Onset of action: Diuresis: ~2 hours
Peak effect: 4-6 hours
Duration: 6-12 hours
Absorption: ~50% to 80%
Distribution: 3.6-7.8 L/kg
Protein binding: 68%
Metabolism: Not metabolized
Bioavailability: 50% to 80%
Half-life elimination: 5.6-14.8 hours
Time to peak: 1-2.5 hours
Excretion: Urine (as unchanged drug).
 
   
 
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