Telmifast
Telmifast Uses, Dosage, Side Effects, Food Interaction and all others data.
Angiotensin II is formed from angiotensin I in a reaction catalyzed by angiotensin-converting enzyme (ACE, kininase II). Angiotensin II is the principal pressor agent of the renin-angiotensin system, with effects that include vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation, and renal reabsorption of sodium. Telmifast blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor in many tissues, such as vascular smooth muscle and the adrenal gland. Its action is therefore independent of the pathways for angiotensin II synthesis.
There is also an AT2 receptor found in many tissues, but AT2 is not known to be associated with cardiovascular homeostasis. Telmifast has a much greater affinity ( > 3,000 fold) for the AT1 receptor than for the AT2 receptor.
Blockade of the renin-angiotensin system with ACE inhibitors, which inhibit the biosynthesis of angiotensin II from angiotensin I, is widely used in the treatment of hypertension. ACE inhibitors also inhibit the degradation of bradykinin, a reaction also catalyzed by ACE. Because telmisartan does not inhibit ACE (kininase II), it does not affect the response to bradykinin. Whether this difference has clinical relevance is not yet known. Telmifast does not bind to or block other hormone receptors or ion channels known to be important in cardiovascular regulation.
Blockade of the angiotensin II receptor inhibits the negative regulatory feedback of angiotensin II on renin secretion, but the resulting increased plasma renin activity and angiotensin II circulating levels do not overcome the effect of telmisartan on blood pressure.
Telmifast is an orally active nonpeptide angiotensin II antagonist that acts on the AT1 receptor subtype. It has the highest affinity for the AT1 receptor among commercially available ARBS and has minimal affinity for the AT2 receptor. New studies suggest that telmisartan may also have PPARγ agonistic properties that could potentially confer beneficial metabolic effects, as PPARγ is a nuclear receptor that regulates specific gene transcription, and whose target genes are involved in the regulation of glucose and lipid metabolism, as well as anti-inflammatory responses. This observation is currently being explored in clinical trials. Angiotensin II is formed from angiotensin I in a reaction catalyzed by angiotensin-converting enzyme (ACE, kininase II). Angiotensin II is the principal pressor agent of the renin-angiotensin system, with effects that include vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation, and renal reabsorption of sodium. Telmifast works by blocking the vasoconstrictor and aldosterone secretory effects of angiotensin II.
| Trade Name | Telmifast |
| Availability | Prescription only |
| Generic | Telmisartan |
| Telmisartan Other Names | Telmisartan |
| Related Drugs | Praluent, Repatha, amlodipine, lisinopril, atorvastatin, metoprolol, losartan, furosemide, hydrochlorothiazide, Xarelto |
| Weight | 80mg, 40mg |
| Type | Tablet |
| Formula | C33H30N4O2 |
| Weight | Average: 514.6169 Monoisotopic: 514.236876224 |
| Protein binding | Highly bound to plasma proteins (>99.5%), mainly albumin and a1-acid glycoprotein. Binding is not dose-dependent. |
| Groups | Approved, Investigational |
| Therapeutic Class | Angiotensin-ll receptor blocker |
| Manufacturer | Pharmasia Ltd |
| Available Country | Bangladesh |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Telmifast is an angiotensin II receptor blocker (ARB) used for treatment of hypertension and Cardiovascular (CV) risk reduction in patients who are used for ACE inhibitors.
Telmifast is also used to associated treatment for these conditions: Cardiovascular Events, Diabetic Nephropathy, Heart Failure, High Blood Pressure (Hypertension)
How Telmifast works
Telmifast interferes with the binding of angiotensin II to the angiotensin II AT1-receptor by binding reversibly and selectively to the receptors in vascular smooth muscle and the adrenal gland. As angiotensin II is a vasoconstrictor, which also stimulates the synthesis and release of aldosterone, blockage of its effects results in decreases in systemic vascular resistance. Telmifast does not inhibit the angiotensin converting enzyme, other hormone receptors, or ion channels. Studies also suggest that telmisartan is a partial agonist of PPARγ, which is an established target for antidiabetic drugs. This suggests that telmisartan can improve carbohydrate and lipid metabolism, as well as control insulin resistance without causing the side effects that are associated with full PPARγ activators.
Dosage
Telmifast dosage
Hypertension: Dosage must be individualized. The usual starting dose of Telmifast tablets is 40 mg once a day. Blood pressure response is dose-related over the range of 20 to 80 mg
Most of the antihypertensive effect is apparent within 2 weeks and maximal reduction is generally attained after 4 weeks. When additional blood pressure reduction beyond that achieved with 80 mg Telmifast is required, adiuretic may be added.
No initial dosage adjustment is necessary for elderly patients or patients with renal impairment, including those on hemodialysis. Patients ondialysismay develop orthostatic hypotension; their blood pressure should be closely monitored.
Cardiovascular Risk Reduction: The recommended dose of Telmifast tablets is 80 mg once a day and can be administered with or without food. It is not known whether doses lower than 80 mg of telmisartan are effective in reducing the risk of cardiovascular morbidity and mortality.
When initiating Telmifast therapy for cardiovascular risk reduction, monitoring of blood pressure is recommended, and if appropriate, adjustment of medications that lower blood pressure may be necessary.
Telmifast tablets may be administered with other antihypertensive agents with or without food.
Side Effects
Most people tolerate telmisartan well. Side effects are usually minor and either require no treatment or can easily be treated by physician. The most common telmisartan side effects include-Upper respiratory infection such as the common cold or flu up to 7 percent of people, Back pain up to 3 percent of people, Diarrhea up to 3 percent of people, Inflammation of the sinuses up to 3 percent of people.
Toxicity
Intravenous LD50 in rats is 150-200 mg/kg in males and 200 to 250 mg/kg in females. Acute oral toxicity is low: no deaths and no changes occurred in rats or dogs at 2000 mg/kg, the highest dose tested. Limited data are available with regard to overdosage in humans. The most likely manifestations of overdosage with telmisartan would be hypotension, dizziness and tachycardia; bradycardia could occur from parasympathetic (vagal) stimulation.
Precaution
Use of drugs that act on the renin-angiotensin system during the second and third trimesters of pregnancy reduces fetal renal function and increases fetal and neonatal morbidity and death. Telmifast may potentially cause extreme low blood pressure or a decrease in kidney function. Hyperkalemia may occur in patients on ARBs, particularly in patients with advanced renal impairment, heart failure, on renal replacement therapy or on potassium supplements, potassium-sparing diuretics, potassium containing salt substitutes or other drugs that increase potassium levels.
Interaction
When certain medicines are taken together, there is a possibility of developing drug interactions. With Telmifast, drugs such as potassium supplements or potassium-sparing diuretics may cause an interaction. When Telmifast was co-administered with digoxin, median increases in digoxin peak plasma concentration (49%) and in through concentration (20%) where observed. Therefore, monitor digoxin levels when initiating, adjusting and discontinuing Telmifast for the purpose of keeping the digoxin level within the therapeutic range. NSAID use may lead to increase risk of renal impairment and loss of antihypertensive effect. Monitor renal function periodically in patients receiving Telmifast and NSAID therapy.
Food Interaction
- Take with or without food. Bioavailability may be slightly reduced by taking telmisartan with food.
[Moderate] GENERALLY AVOID: Moderate-to-high dietary intake of potassium, especially salt substitutes, may increase the risk of hyperkalemia in some patients who are using angiotensin II receptor blockers (ARBs).
ARBs can promote hyperkalemia through inhibition of angiotensin II-induced aldosterone secretion.
Patients with diabetes, heart failure, dehydration, or renal insufficiency have a greater risk of developing hyperkalemia.
MANAGEMENT: Patients should receive dietary counseling and be advised to not use potassium-containing salt substitutes or over-the-counter potassium supplements without consulting their physician.
If salt substitutes are used concurrently, regular monitoring of serum potassium levels is recommended.
Patients should also be advised to seek medical attention if they experience symptoms of hyperkalemia such as weakness, irregular heartbeat, confusion, tingling of the extremities, or feelings of heaviness in the legs.
Telmifast Alcohol interaction
[Moderate]
Many psychotherapeutic and CNS-active agents (e.g., anxiolytics, sedatives, hypnotics, antidepressants, antipsychotics, opioids, alcohol, muscle relaxants) exhibit hypotensive effects, especially during initiation of therapy and dose escalation.
Coadministration with antihypertensives and other hypotensive agents, in particular vasodilators and alpha-blockers, may result in additive effects on blood pressure and orthostasis.
Caution and close monitoring for development of hypotension is advised during coadministration of these agents.
Some authorities recommend avoiding alcohol in patients receiving vasodilating antihypertensive drugs.
Patients should be advised to avoid rising abruptly from a sitting or recumbent position and to notify their physician if they experience dizziness, lightheadedness, syncope, orthostasis, or tachycardia.
Telmifast Drug Interaction
Moderate: aspirin, aspirin, empagliflozin, pregabalinUnknown: ubiquinone, rosuvastatin, apixaban, omega-3 polyunsaturated fatty acids, sitagliptin, atorvastatin, metoprolol, metoprolol, acetaminophen, levothyroxine, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol, rivaroxaban, cetirizine
Telmifast Disease Interaction
Major: diabetes, angioedema, hypotensionModerate: CHF, hyperkalemia, renal artery stenosis, renal impairment, renal/liver disease
Volume of Distribution
- 500 L
Elimination Route
Absolute bioavailability depends on dosage. Food slightly decreases the bioavailability (a decrease of about 6% is seen when the 40-mg dose is administered with food).
Half Life
Bi-exponential decay kinetics with a terminal elimination half-life of approximately 24 hours.
Clearance
- >800 mL/min
Elimination Route
Following either intravenous or oral administration of 14C-labeled telmisartan, most of the administered dose (>97%) was eliminated unchanged in feces via biliary excretion; only minute amounts were found in the urine (0.91% and 0.49% of total radioactivity, respectively).
Pregnancy & Breastfeeding use
Telmifast has been assigned to pregnancy categories C (use during first trimester) by the FDA. When pregnancy is detected or expected, Telmifast should be discontinued as soon as possible. The use of drugs that act directly on the RAA system during the second and third trimesters has been associated with fetal and neonatal injury, including hypotension, neonatal skull hypoplasia, anuria, reversible or irreversible renal failure and death. There are no data on the excretion of Telmifast into human milk, due to the potential for serious adverse effects in the nursing infant, a decision should be made to discontinue nursing or discontinue the drug.
Contraindication
Telmifast is contraindicated in conditions like Pregnancy, Adjunct in treatment of opioid dependence, Dry or painful cough. Telmifast is also contraindicated in patients with known hypersensitivity to telmisartan.
Special Warning
Renal Impairment: Severe impairment or on haemodialysis: Initially, 20 mg once daily.
Hepatic Impairment: Mild to moderate: Max: 40 mg once daily. Severe: Contraindicated.
Acute Overdose
Symptoms: Hypotension, bradycardia, tachycardia, dizziness, acute renal failure and elevated serum creatinine.
Management: Supportive and symptomatic treatment. Induction of emesis and/or gastric lavage. Activated charcoal may be useful. Salt and volume replacement should be given immediately if hypotension occurs and place patient in supine position.
Storage Condition
Store in a cool and dry place, protected from light. Keep out of children’s reach
Innovators Monograph
You find simplified version here Telmifast
Telmifast contains Telmisartan see full prescribing information from innovator Telmifast Monograph, Telmifast MSDS, Telmifast FDA label
FAQ
What is Telmifast used for?
Telmifast is used to treat high blood pressure (hypertension). Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems.
How safe is Telmifast?
Telmifast is a safe drug when used as directed by your doctor with careful monitoring. It lowers blood pressure and protects the heart and kidneys, but in rare cases can lead to heart and kidney problems.
What are the common side effects of Telmifast?
Common side effects are include:
- Changes in vision.
- dizziness, lightheadedness, or fainting.
- fast heartbeat.
- large hives.
- painful urination or changes in urinary frequency.
- swelling in the hands, lower legs, and feet.
Does Telmifast affect the eyes?
This drug can cause certain eye problems. If left untreated, this can lead to lasting eyesight loss. If eye problems happen, signs like change in eyesight or eye pain most often happen within hours to weeks of starting this drug
How long should Telmifast be taken?
the antihypertensive effect of once-daily administration of Telmifast maintained for the full 24-hour dose interval.
Is it safe to drink alcohol with Telmifast?
It is best to limit your intake of alcohol while taking this drug. Alcohol can increase the risk for low blood pressure and dizziness. If the blood pressure drops too low, you may feel dizzy or faint, in some cases falls or fainting may occur.
Is Telmifast safe in pregnancy?
Telmifast is contraindicated in pregnancy, adverse effects have been reported in human pregnancies.
Is Telmifast safe in breastfeeding?
Because no information is available on the use of Telmifast during breastfeeding, an alternate drug may be preferred, especially while nursing a newborn or preterm infant.
Can I drive after taking Telmifast?
Some people feel dizzy or tired when taking Telmifast Tablets. If you feel dizzy or tired, do not drive or operate machinery.
What is the best time to take Telmifast?
Telmifast administered at bedtime, as opposed to morning dosing, improved the sleep time-relative blood pressure decline toward a more dipper pattern without loss in 24-hour efficacy.
How long does Telmifast stay in my system?
Telmifast has the longest half-life of about 24 hour.
Does Telmifast work immediately?
The onset of antihypertensive activity occurs within 3 hours, with a maximal reduction by approximately 4 weeks.At doses antihypertensive effect of once-daily administration of telmisartan maintained for the full 24-hour dose interval.
Can I take Telmifast every other day?
You take Telmifast a tablets every day until your doctor tells you otherwise.
What happens if I stop taking Telmifast?
If you stop taking Telmifast suddenly can cause your blood pressure to spike. This can increase your risk for heart attack or stroke.
Is Telmifast safe for kidneys?
Telmifast effectively and safely reduced blood pressure and brought about regression of proteinuria in diabetic and nondiabetic, hypertensive, proteinuric patients with chronic kidney disease, even in those with mild-to-moderate chronic renal failure.
Is Telmifast bad for liver?
Telmifast has yet to be linked to instances of acute liver injury.
Why is Telmifast taken at night?
Telmifast administered at bedtime, as opposed to morning dosing, improved the sleep time-relative blood pressure decline toward a more dipper pattern without loss in 24-hour efficacy.
Does Telmifast reduce cholesterol?
Telmifast has been demonstrated that telmisartan also lowers the levels of total cholesterol.
Does Telmifast cause memory loss?
Telmifast may causes spatial working memory impairment with glial activation.
Does Telmifast increase uric acid?
Telmifast may causes showed no effects on plasma uric acid level.
