Probertan

Probertan Uses, Dosage, Side Effects, Food Interaction and all others data.

Probertan is an angiotensin II receptor antagonist. It blocks the vasoconstricting and aldosterone-secreting effects of angiotensin II by binding to AT1 receptors.

Probertan is an angiotensin receptor blocker used to treat hypertension and diabetic nephropathy. It has a long duration of action as it is usually taken once daily and a wide therapeutic index as doses may be as low as 150mg daily but doses of 900mg/day were well tolerated in healthy human subjects.

Trade Name Probertan
Availability Prescription only
Generic Irbesartan
Irbesartan Other Names Irbesartan
Related Drugs amlodipine, lisinopril, metoprolol, losartan, furosemide, hydrochlorothiazide, ramipril, captopril, enalapril, benazepril
Type
Formula C25H28N6O
Weight Average: 428.5294
Monoisotopic: 428.232459548
Protein binding

Irbesartan is 90% protein bound in plasma, mainly to albumin and α1-acid glycoprotein.

Groups Approved, Investigational
Therapeutic Class Angiotensin-ll receptor blocker
Manufacturer
Available Country Peru
Last Updated: September 19, 2023 at 7:00 am
Probertan
Probertan

Uses

Treatment of essential hypertension. Treatment of renal disease in patients with hypertension and type 2 diabetes mellitus as part of an antihypertensive drug regimen.

Probertan is also used to associated treatment for these conditions: Diabetic Nephropathy, High Blood Pressure (Hypertension)

How Probertan works

Probertan prevents angiotensin II binding to the AT1 receptor in tissues like vascular smooth muscle and the adrenal gland. Probertan and its active metabolite bind the AT1 receptor with 8500 times more affinity than they bind to the AT2 receptor. Probertan's prevention of angiotensin II binding causes vascular smooth muscle relaxation and prevents the secretion of aldosterone, lowering blood pressure.

Angiotensin II would otherwise bind to the AT1 receptor, inducing vasoconstriction and aldosterone secretion, raising blood pressure.

Dosage

Probertan dosage

Adult: The usual recommended initial and maintenance dose is Probertan 150 mg once daily, withor without food. Probertan at a dose of 150 mg once daily generally provides a better 24 hourblood pressure control than 75 mg. However, initiation of therapy with Probertan 75 mg couldbe considered, particularly in haemodialysed patients and in the elderly over 75 years.In patients insufficiently controlled with Probertan 150 mg once daily, the dose of Probertancan be increased to Probertan 300 mg, or other anti-hypertensive agents can be added. In particular, the addition of a diuretic such as hydrochlorothiazide has been shown to have anadditive effect with Probertan.In hypertensive type 2 diabetic patients, therapy should be initiated at Probertan 150 mgonce daily and titrated up to Probertan 300 mg once daily as the preferred maintenance dosefor treatment of renal disease.The demonstration of renal benefit of Probertan in hypertensive type 2 diabetic patients is basedon studies where Probertan was used in addition to other antihypertensive agents, as needed, toreach target blood pressure.

Elderly: although consideration should be given to initiating therapy with Probertan 75 mg in patients over 75 years of age, dosage adjustment is not usually necessary for the elderly

Paediatric: Probertan is not recommended for use in children and adolescents due toinsufficient data on safety and efficacy.

Side Effects

Diarrhoea, fatigue, dyspepsia or heartburn, dizziness, orthostatic hypotension, nausea, vomiting, musculoskeletal pain, thrombocytopaenia, hyperkalaemia, elevated serum creatinine.

Toxicity

The oral TDLO in humans is 30mg/kg/6W.

Symptoms of overdose include hypotension and tachycardia or bradycardia. Terlipressin may be given to treat hypotension and tachycardia if conventional vasopressors fail to control blood pressure.

Precaution

Patients with unilateral or bilateral renal artery stenosis, depletion of intravascular volume, aortic or mitral stenosis, or obstructive hypertrophic cardiomyopathy. Renal impairment. Lactation.

Interaction

Diuretics and other antihypertensive agents: prior treatment with high dose diuretics may result in volume depletion and a risk of hypotension when initiating therapy with Probertan.

Potassium supplements and potassium-sparing diuretics: based on experience with the use of other drugs that affect the renin-angiotensin system, concomitant use of potassiumsparing diuretics, potassium supplements, salt substitutes containing potassium or other drugs that may increase serum potassium levels (e.g. heparin) may lead to increases in serum potassium and is, therefore, not recommended.

Lithium: reversible increases in serum lithium concentrations and toxicity have been reported during concomitant administration of lithium with angiotensin converting enzyme inhibitors. Similar effects have been very rarely reported with irbesartan so far. Therefore, this combination is not recommended. If the combination proves necessary, careful monitoring of serum lithium levels is recommended.

Non-steroidal anti-inflammatory drugs: When angiotensin II antagonists are administered simultaneously with non-steroidal anti- inflammatory drugs (i.e. selective COX-2 inhibitors, acetylsalicylic acid > 3 g/day and non-selective NSAIDs), attenuation of the antihypertensive effect may occur. Additional information on irbesartan interactions: In clinical studies, the pharmacokinetic of irbesartan is not affected by hydrochlorothiazide. Probertan is mainly metabolised by CYP2C9 and to a lesser extent by glucuronidation. No significant pharmacokinetic or pharmacodynamic interactions were observed when irbesartan was coadministered with warfarin, a drug metabolised by CYP2C9. The effects of CYP2C9 inducers such as rifampicin on the pharmacokinetic of irbesartan have not been evaluated. The pharmacokinetic of digoxin was not altered by coadministration of irbesartan.

Food Interaction

  • Take with or without food. The absorption is unaffected by 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.

Volume of Distribution

The volume of distribution of irbesartan is 53-93L.

Elimination Route

Probertan is 60-80% bioavailable with a Tmax of 1.5-2hours. Taking irbesartan with food does not affect the bioavailability.

In one study, healthy subjects were given single or multiple oral doses of 150mg, 300mg, 600mg, and 900mg of irbesartan. A single 150mg dose resulted in an AUC of 9.7±3.0µg\•hr/mL, a Tmax of 1.5 hours, a half life of 16±7 hours, and a Cmax of 1.9±0.4µg/mL. A single 300mg dose resulted in an AUC of 20.0±5.2µg\•hr/mL, a Tmax of 1.5 hours, a half life of 14±7 hours, and a Cmax of 2.9±0.9µg/mL. A single 600mg dose resulted in an AUC of 32.6±11.9µg\•hr/mL, a Tmax of 1.5 hours, a half life of 14±8 hours, and a Cmax of 4.9±1.2µg/mL. A single 900mg dose resulted in an AUC of 44.8±20.0µg\•hr/mL, a Tmax of 1.5 hours, a half life of 17±7 hours, and a Cmax of 5.3±1.9µg/mL.

Multiple 150mg doses resulted in an AUC of 9.3±3.0µg\•hr/mL, a Tmax of 1.5 hours, a half life of 11±4 hours, and a Cmax of 2.04±0.4µg/mL. Multiple 300mg doses resulted in an AUC of 19.8±5.8µg\•hr/mL, a Tmax of 2.0 hours, a half life of 11±5 hours, and a Cmax of 3.3±0.8µg/mL. Multiple 600mg doses resulted in an AUC of 31.9±9.7µg\•hr/mL, a Tmax of 1.5 hours, a half life of 15±7 hours, and a Cmax of 4.4±0.7µg/mL. Multiple 900mg doses resulted in an AUC of 34.2±9.3µg\•hr/mL, a Tmax of 1.8 hours, a half life of 14±6 hours, and a Cmax of 5.6±2.1µg/mL.

Half Life

The terminal elimination half life of irbesartan is 11-15 hours.

Clearance

Total plasma clearance of irbesartan is 157-176mL/min while renal clearance is 3.0-3.5mL/min.

Elimination Route

20% of a radiolabelled oral dose of irbesartan is recovered in urine, and the rest is recovered in the feces. 10

Pregnancy & Breastfeeding use

Pregnancy: Probertan is contraindicated in the second and third trimesters of pregnancy. In the second and third trimesters, substances that act directly on the renin-angiotensin-system can cause foetal or neonatal renal failure, foetal skull hypoplasia and even foetal death. As precautionary measure, irbesartan should preferably not be used during first trimester of pregnancy. A switch to a suitable alternative treatment should be carried out in advance of a planned pregnancy. If pregnancy is diagnosed, irbesartan should be discontinued as soon as possible, skull and renal function should be checked with echography if, inadvertently, the treatment was taken for a long period.

Lactation: Probertan is contraindicated during lactation. It is not known whether irbesartan is excreted in human milk. Probertan is excreted in the milk of lactating rats. Precautions: Intravascular volume depletion: symptomatic hypotension, especially after the first dose, may occur in patients who are volume and/or sodium depleted by vigorous diuretic therapy, dietary salt restriction, diarrhoea or vomiting. Such conditions should be corrected before the administration of Probertan.

Contraindication

Concomitant use with aliskiren in patients with diabetes and renal impairment (GFR <60 ml/min). Pregnancy.

Special Warning

Renal impairment: no dosage adjustment is necessary in patients with impaired renal function. A lower starting dose of Probertan 75 mg should be considered for patients undergoing haemodialysis. Intravascular volume depletion: volume and/or sodium depletion should be corrected prior to administration of Probertan.

Hepatic impairment: no dosage adjustment is necessary in patients with mild to moderate hepatic impairment. There is no clinical experience in patients with severe hepatic impairment.

Hypertensive patients with type 2 diabetes and renal disease: the effects of irbesartan both on renal and cardiovascular events were not uniform across all subgroups, in an analysis carried out in the study with patients with advanced renal disease. In particular, they appeared less favourable in women and non-white subjects.

Hyperkalaemia: as with other drugs that affect the renin-angiotensin-aldosterone system, hyperkalaemia may occur during the treatment with Probertan, especially in the presence of renal impairment, overt proteinuria due to diabetic renal disease, and/or heart failure. Close monitoring of serum potassium in patients at risk is recommended.

Aortic and mitral valve stenosis, obstructive hypertrophic cardiomyopathy: as with other vasodilators, special caution is indicated in patients suffering from aortic or mitral stenosis, or obstructive hypertrophic cardiomyopathy.

Primary aldosteronism: patients with primary aldosteronism generally will not respond to anti-hypertensive drugs acting through inhibition of the renin-angiotensin system. Therefore, the use of Probertan is not recommended.

General: in patients whose vascular tone and renal function depend predominantly on the activity of the renin-angiotensinaldosterone system (e.g. patients with severe congestive heart failure or underlying renal disease, including renal artery stenosis), treatment with angiotensin converting enzyme inhibitors or angiotensin-II receptor antagonists that affect this system has been associated with acute hypotension, azotaemia, oliguria, or rarely acute renal failure. As with any anti-hypertensive agent, excessive blood pressure decrease in patients with ischaemic cardiopathy or ischaemic cardiovascular disease could result in a myocardial infarction or stroke.

Acute Overdose

Experience in adults exposed to doses of up to 900 mg/day for 8 weeks revealed no toxicity. The most likely manifestations of overdosage are expected to be hypotension and tachycardia; bradycardia might also occur from overdose. No specific information is available on the treatment of overdosage with Probertan. The patient should be closely monitored, and the treatment should be symptomatic and supportive. Suggested measures include induction of emesis and/or gastric lavage. Activated charcoal may be useful in the treatment of overdosage. Probertan is not removed by haemodialysis.

Storage Condition

Store in a cool and dry place, protected from light.

Innovators Monograph

You find simplified version here Probertan

Probertan contains Irbesartan see full prescribing information from innovator Probertan Monograph, Probertan MSDS, Probertan FDA label

FAQ

What is Probertan used for?

Probertan is a medication used to treat high blood pressure, heart failure, and diabetic kidney disease. It is a reasonable initial treatment for high blood pressure

How safe is Probertan?

Probertan is generally safe to take for a long time. In fact, it works best when you take it for a long time. Taking Probertan for a long time can sometimes cause your kidneys to not work as well as they should.

How dose Probertan work ?

Probertan works by blocking a substance in the body that causes blood vessels to tighten. As a result, irbesartan relaxes the blood vessels.

What are the common side effects of Probertan?

The common side effects of Probertan are dizziness, headache, feeling or being sick (nausea or vomiting) and low blood pressure - but they're usually mild and short-lived. If you get severe diarrhoea or vomiting from a stomach bug or illness, tell your doctor.

Is Probertan safe during pregnancy?

Do not take Probertan if you are pregnant. If you become pregnant while you are taking Probertan, stop taking Probertan and call your doctor immediately. Probertan may cause death or serious injury to the fetus when taken in the last 6 months of pregnancy.

Is Probertan safe during breastfeeding?

Small amounts of irbesartan may get into breast milk. This can cause low blood pressure in the baby. Talk to your doctor, as other medicines might be better while you are breastfeeding.

Can I drink alcohol with Probertan?

During the first few days of taking Probertan or after a dose increase, it is best to stop drinking alcohol until you see how the medicine affects you.

When should be taken of Probertan?

Your doctor may suggest that you take your first dose before bedtime, because it can make you dizzy. After the very first dose, you can take Probertan at any time of day. Try to take it at the same time every day.

How many Probertan can I take a day?

Take Probertan tablets once a day.

Can I take Probertan on an empty stomach?

You can take Probertan tablets with or without food.

How long does Probertan take to work?

Probertan starts to work after about 3 to 6 hours to reduce high blood pressure but it may take up to 4 to 6 weeks for full effect.

What is the half life of Probertan?

The terminal elimination half-life of Probertan is 11-15 hours. Steady- state plasma concentrations are attained within 3 days after initiation of a once-daily dosing regimen.

Can I take Probertan for a long time?

Probertan is generally safe to take for a long time. In fact, Probertan works best when you take it for a long time. Taking Probertan for a long time can sometimes cause your kidneys to not work as well as they should.

Should I stop taking Probertan?

Stopping it may cause your blood pressure to rise - and this can increase your chances of having a heart attack or stroke.

Who should not take Probertan ?

You may also need to avoid taking Probertan with aliskiren if you have kidney disease. Do not use if you are pregnant. Stop using and tell your doctor right away if you become pregnant. If you have diabetes, do not take Probertan.

What happens if I miss a dose?

Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.

What happens if I overdose?

Seek emergency medical attention. Overdose symptoms may include fast heartbeats or fainting.

What should I avoid while taking Probertan ?

Do not use potassium supplements or salt substitutes, unless your doctor has told you to. Avoid getting up too fast from a sitting or lying position, or you may feel dizzy.

Can Probertan affect my fertility?

Speak to a pharmacist or your doctor before taking it if you're trying to get pregnant. Probertan won't affect any type of contraception.

Can Probertan affects my heart ?

Stopping it may cause your blood pressure to rise - and this can increase your chances of having a heart attack or stroke.

Can Probertan affect my kidneys?

Using irbesartan can worsen your kidney function. Taking Probertan for a long time can sometimes cause your kidneys to not work as well as they should.

Can Probertan affects my liver?

Probertan is associated with a low rate of transient serum aminotransferase elevations and has been linked to rare instances of acute liver injury.

Can Probertan make my gain weight?

Rapid weight gain is common side effect of the Probertan.

*** Taking medicines without doctor's advice can cause long-term problems.
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