Tikal

Description

Tikal is an antihypertensive drug that contains two active ingredients: Telmisartan and Amlodipine (the association of an AT1 receptor antagonist of IIA and a calcium channel blocker).

Telmisartan is a specific and orally effective angiotensin II AT1 receptor antagonist that selectively binds to the AT1 receptor (long-lasting binding) and has no affinity for AT2 receptors and other less characterized AT receptors. Telmisartan reduces plasma levels of aldosterone, does not inhibit human plasma renin or block ion channels, does not inhibit angiotensin-converting enzyme (quinine II), which also degrades bradykinin, therefore it is not expected to enhance the Bradykinin-mediated adverse effects. In man, one dose of Telmisartan virtually completely inhibits the increase in blood pressure caused by angiotensin II. The inhibitory effect is maintained for 24 hours and can still be detected after 48 hours. After the first dose of Telmisartan, the antihypertensive activity gradually becomes evident within 3 hours. The maximum reduction in blood pressure is usually reached 4 weeks after starting treatment and is maintained during long-term therapy. After abrupt discontinuation of treatment with Telmisartan, blood pressure gradually returns to pre-treatment values ​​over a period of several days, with no evidence of rebound hypertension.

Amlodipine is a drug belonging to the group of dihydropyridines, which acts as a long-acting calcium channel blocker, used in medicine as an antihypertensive and in the treatment of angina pectoris.

Amlodipine is well absorbed after oral administration, reaching maximum blood concentrations 6-12 hours after administration, its absolute bioavailability is 64-80% and the plasma elimination half-life is 35-50 hours.

Both active ingredients work together to provide an adequate reduction in blood pressure, higher response and control rates, and offer a more favorable safety profile, compared to treatment with Telmisartan or Amlodipine monotherapy.

Indications

Tikal is indicated for the treatment of hypertension, alone or in combination with other antihypertensive agents. It can also be used as initial therapy in patients who need multiple drugs to achieve their blood pressure goals.


Posology

The initial dose of Tikal is 40 / 5mg 1 time a day. Patients requiring greater reductions in blood pressure may initially receive: Tikal 80 / 5mg 1 time a day. If additional reduction in blood pressure is required after at least 2 weeks of treatment, the dose can be titrated up to a maximum of 80 / 10mg 1 time a day. Tikal can be administered with other antihypertensive medications and can be taken with or without food.

Initial treatment: a patient can be started on Tikal if it is considered unlikely that control of their blood pressure can be obtained with a single agent. Replacement treatment: patients receiving Telmisartan and Amlodipine in separate tablets may instead receive Tikal with the same doses of the components in 1 tablet once a day. Addition treatment: Tikal can be administered in patients in whom blood pressure is not adequately controlled with Amlodipine or Telmisartan monotherapy. Patients treated with Amlodipine 10 mg experiencing any dosage limitations or side effects, such as edema, may be switched to Tikal 40 / 5mg 1 time daily, reducing the Amlodipine dose without decreasing the anticipated general antihypertensive response.

No dosage adjustment is required for patients with mild to moderate renal impairment, and should be titrated in those patients with severe renal impairment.

In patients with mild to moderate hepatic dysfunction, Tikal should be administered with caution. For Telmisartan the dosage should not exceed 40mg 1 time a day. No dosage adjustment is necessary in the elderly. Tikal is not recommended for use in patients under 18 years of age due to a lack of information on safety and efficacy.

 

Side effects

 

Common (1 in 10 people): dizziness, ankle swelling.

Uncommon (1 in 100 people): migraine, tingling or numbness in the hands or feet, vertigo, bradycardia, palpitations, hypotension, orthostatic hypotension, flushing, cough, diarrhea, nausea, muscle spasms, tiredness.

Rare (1 in 1,000 people): urinary bladder infection, depression.

Drug interactions

No interactions have been observed between the 2 components of this fixed combination. The lowering effect of Tikal blood pressure can be increased with the concomitant use of other antihypertensive agents. Agents with hypotensive potential: Based on their pharmacological properties, the drugs that can potentiate the hypotensive effect of all antihypertensives, including Tikal are for example Baclofen and Amifostine. Furthermore, orthostatic hypotension can be aggravated by alcohol, barbiturates, narcotics, or antidepressants. Corticosteroids (systemic): reduction of the antihypertensive effect. Interactions with Telmisartan: Telmisartan may increase the hypotensive effect of other antihypertensive agents. Concomitant administration of Telmisartan does not involve clinically significant interactions with digoxin, warfarin, hydrochlorothiazide, glibenclamide, ibuprofen, paracetamol, simvastatin, and amlodipine. For digoxin, a 20% increase in the mean plasma level has been observed, therefore monitoring of its plasma levels should be considered. Reversible increases in serum lithium concentrations and toxicity have been reported during concomitant administration of lithium with angiotensin-converting enzyme inhibitors. Cases have also been reported with angiotensin II receptor antagonists, including Telmisartan. Therefore, it is advisable to monitor serum lithium levels during concomitant use. Compounds that affect the renin-angiotensin-aldosterone system, such as Telmisartan, may have synergistic effects. Interactions with Amlodipine: Concomitant use requires caution. CYP3A4 inhibitors: Diltiazem inhibits amlodipine metabolism, probably via CYP3A4 (the plasma concentration increases by approximately 50% and the effect of amlodipine is increased). The possibility that more potent CYP3A4 inhibitors (Ketoconazole, itraconazole, ritonavir) may increase the plasma concentration of amlodipine to a greater extent than diltiazem cannot be excluded. CYP3A4 inducers (anticonvulsant agents (Carbamazepine, Phenobarbital, Phenytoin, Phosphenytoin, Primidone), Rifampicin, Hypericum perforatum): Concomitant administration with these agents may lead to reduced plasma levels of amlodipine. Clinical monitoring is required, with possible adjustments in the amlodipine dosage during treatment with the inducer and after its withdrawal. Other concomitant uses: As monotherapy, amlodipine has been safely administered with thiazide diuretics, beta-blockers, ACE inhibitors, long-acting nitrates, sublingual nitroglycerin, NSAIDs, antibiotics, and oral hypoglycemic drugs. Concomitant administration of amlodipine with atorvastatin, digoxin, warfarin, or cyclosporine has no significant effect on the pharmacokinetics or pharmacodynamics of these medicinal products.

 

 

Composition

Tikal 40/5

Each coated tablet contains::

Telmisartan 40mg

Amlodipine (as amlodipine besilate) 5mg

C.S.P. excipients

Tikal 40/10

Each coated tablet contains::

Telmisartan 40mg

Amlodipine (as amlodipine besilate) 10mg

C.S.P. excipients

Tikal 80/5

Each coated tablet contains::

Telmisartan 80mg

Amlodipine (as amlodipine besilate) 5mg

C.S.P. excipients

Tikal 80/10

Each coated tablet contains::

Telmisartan 80mg

Amlodipine (as amlodipine besilate) 10mg

C.S.P. excipients


Administration route

Oral


Presentation

Tikal 40/5 box containing 10 and 30 coated tablets.

Tikal 40/10 box containing 10 and 30 coated tablets.

Tikal 80/5 box containing 10 and 30 coated tablets.

Tikal 80/10 box containing 10 and 30 coated tablets.


Storage

Store below 30 °C. Protect it from light and moisture.


Contraindications

Tikal is contraindicated in case of  hypersensitivity to the active substances, or to any of the excipients, hypersensitivity to derivatives of dihydropyridines, second and third trimester of pregnancy, lactation, biliary obstructive disorders, severe liver dysfunction, cardiogenic shock, severe hypotension, hemodynamically unstable heart failure after heart attack. myocardium.

Warning

Keep out of the reach of children. Sale under prescription.

Cautions

Tikal should be used with caution in patients who are receiving NSAIDs together, as NSAIDs have been associated with potential kidney failure in dehydrated patients. If the use of Tikal and an NSAID is necessary, the patient must be adequately hydrated and monitored for renal function at the start of treatment. In addition to this, a reduced effect of antihypertensives, including Telmisartan has been reported by the inhibition of vasodilator prostaglandins during concomitant treatment with NSAIDs.