Indications for Telmisartan
Indicated for the treatment of essential hypertension.
Telmisartan dosage
1. Telmisartan should be administered orally on an individualized basis. The usual initial dose is 40 mg once per mouth.
2. In the dose range of 20-80 mg, the antihypertensive efficacy of Telmisartan is dose-dependent, i.e., if the desired blood pressure is not achieved, the dose may be increased, up to a maximum dose of 80 mg once daily. since Telmisartan does not reach its maximum efficacy until 4-8 weeks after the beginning of the treatment course, care should be taken to make any adjustments to the dosage after this period of time.
Major adverse reactions to Telmisartan
1. Adverse reactions to the drug are rare and mild, if any, and generally do not require discontinuation of the drug.
2. Placebo-controlled clinical trials have shown that adverse reactions to Telmisartan are not significantly different from placebo. Adverse reactions were not related to patient gender, age, or race. Adverse reactions observed in the trials included infections (e.g., urinary tract infections and upper respiratory tract infections), abdominal pain, diarrhea, dyspepsia, eczema-like skin lesions, arthritis, and chest pain, but the causal relationship between these adverse reactions and the drug is uncertain.
3. The incidence of hypotension is low. The drug may cause excessive lowering of blood pressure, mainly manifested as dizziness, blackness before the eyes, cold sweat, pallor and other symptoms of low blood pressure when suddenly get up, most of them are transient, and some of the serious cases need to lie down and rest for a few moments before gradually improving. Some severe cases need to lie down and rest for a few moments to get better. Those with excessive lowering of blood pressure need to reduce the dose of drugs.
4. Hyperkalemia: blood potassium >5.5 mmol/L. The drug can cause aldosterone to reduce potassium excretion, so the body potassium increases, hyperkalemia occurs, that is, the blood potassium >5.5 mmol/L, this time can be given to lower the potassium symptomatic treatment or stop the drug.
5. Angioneurotic edema and urticaria have been reported, but they are rare. It may be an allergic reaction to the drug, if it occurs, it is necessary to stop the drug immediately and consult the doctor in time, the mild cases can be recovered, while the serious cases need to be resuscitated.
Contraindications to Telmisartan
1. It is contraindicated in case of hypersensitivity to any of the components of the drug.
2. It is contraindicated in pregnant and lactating women.
3. Because Telmisartan is mainly excreted through the bile, it is contraindicated in patients with biliary obstructive diseases and severe hepatic impairment.
Telmisartan precautions
1. Patients with hepatic insufficiency: because Telmisartan is mainly excreted through the bile, it should not be used in patients with cholestasis, biliary obstruction and severe hepatic insufficiency, which have reduced hepatic clearance of telmisartan. telmisartan should be used with caution in patients with mild to moderate hepatic impairment.
2. Renal vascular hypertension: Bilateral renal artery stenosis or only a single renal artery and the occurrence of renal artery stenosis in patients with the use of this drug will increase the risk of severe hypotension and renal insufficiency.
3. Renal impairment and renal transplantation patients: may cause renal impairment patients blood potassium and blood creatine levels increased, so the use of the drug should be monitored during the blood potassium and renal function. There is no experience with the latter drug.
4. Patients with hypovolemia and hyponatremia (blood sodium <135 mmol/L) are susceptible to symptoms of symptomatic hypotension such as dizziness, blackness before the eyes, and cold sweating when taking timosartan, so attention should be paid to correcting hypovolemia and hyponatremia prior to taking this drug.
5. As with other vasodilators, Telmisartan should be used with caution in patients with aortic or mitral stenosis or hypertrophic obstructive cardiomyopathy because of the serious consequences of syncope and loss of consciousness.
6.Telmisartan can cause hyperkalemia, especially in the elderly, renal insufficiency or with potassium diuretics should be especially careful; thiazide diuretics (such as hydrochlorothiazide) and the drug has synergistic antihypertensive effect; the drug can enhance the antihypertensive effect of other antihypertensive drugs; the drug can increase the blood concentration of digoxin and lead to digoxin intoxication, the two should be monitored in the latter when the two are used in combination; the drug can increase the toxic reaction of lithium; ephedrine can be used with caution, and can be used with caution in patients with aortic valve or mitral valve stenosis or hypertrophic obstructive cardiomyopathy. Lithium toxicity; ephedrine and pseudoephedrine sympathomimetic activity can make the drug’s antihypertensive effect is weakened; with warfarin, can cause the latter blood concentration of the trough value of a slight decrease.
Telmisartan powder Chemical Properties
Melting point 261-263°C
Boiling point 771.9±70.0 °C(Predicted)
density 1.16
RTECS DV2037500
storage temp. 2-8°C
solubility DMSO: >5 mg/mL at 60 °C
form solid
pka 3.86±0.36(Predicted)
color white
Water Solubility insoluble
Merck 14,9129
BCS Class 2
Stability: Hygroscopic
InChIKey RMMXLENWKUUMAY-UHFFFAOYSA-N
SMILES C1(C2=CC=C(CN3C(CCC)=NC4=C(C)C=C(C5N(C)C6=CC=CC=C6N=5)C=C43)C=C2)=CC=CC=C1C(O)=O
CAS DataBase Reference 144701-48-4(CAS DataBase Reference)
More Introduction:https://en.wikipedia.org/wiki/Telmisartan
