IRBESARTAN

Drugs in Pregnancy and Lactation.

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Name: IRBESARTAN
Class: Antihypertensive
Risk Factor:    CM*

Fetal Risk Summary

Irbesartan is a selective angiotensin II receptor antagonist that is used either alone, or in combination with other antihypertensive agents, for the treatment of hypertension. Irbesartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by preventing angiotensin II from binding to AT1 receptors.

Reproduction studies have been conducted in rats and rabbits during pregnancy (1). In the pregnant rat, doses approximately equal to or higher than the maximum recommended human dose of 300 mg/day on a body surface area basis (MRHD) were associated with increased incidences of renal pelvic cavitation, hydroureter and/or absence of renal papilla. At 4 times the MRHD, subcutaneous edema was observed in the fetuses. The anomalies appeared to be related to late, rather than early, gestational exposure (1). Doses approximately 1.5 times the MRHD in pregnant rabbits produced maternal mortality and abortion. Surviving rabbits had a slight increase in early resorptions (1). No adverse effects on fertility or reproductive performance were seen in male and female rats at an oral dose about 5 times the MRHD (1).

It is not known if irbesartan crosses the human placenta to the fetus. The molecular weight (about 429) is low enough, however, that transfer to the fetus should be expected. The drug does cross the placentas of rats and rabbits in late gestation (1).

No reports describing the use of irbesartan during human pregnancy have been located. The antihypertensive mechanisms of action of irbesartan and angiotensin converting enzyme (ACE) inhibitors are very close. That is, the former selectively blocks the binding of angiotensin II to AT1 receptors, whereas the latter prevents the formation of angiotensin II itself. Therefore, use of this drug during the 2nd and 3rd trimesters may cause teratogenicity and severe fetal and neonatal toxicity that is identical to that seen with ACE inhibitors (e.g., see Captopril or Enalapril). Fetal toxic effects may include anuria, oligohydramnios, fetal hypocalvaria, intrauterine growth retardation, prematurity, and patent ductus arteriosus. Anuria-associated oligohydramnios may produce fetal limb contractures, craniofacial deformation, and pulmonary hypoplasia. Severe anuria and hypotension, that is resistant to both pressor agents and volume expansion, may occur in the newborn following in utero exposure to irbesartan. Newborn renal function and blood pressure should be closely monitored.

[*Risk factor DM if used in 2nd or 3rd trimesters.]

Breast Feeding Summary

No reports describing the use irbesartan during human lactation have been located. The agent is found in the milk of lactating rats (1). Because of the relatively low molecular weight (about 429), excretion into human breast milk should also be expected. The effects of this exposure on a nursing infant are unknown. The American Academy of Pediatrics, however, considers ACE inhibitors, a closely related group of antihypertensive agents, to be compatible with breast feeding (see Captopril or Enalapril).

Reference

  • Product information. Avapro. Bristol-Myers Squibb, 2000.

    Index

    Q&A about Irbesartan

    Bren
    anyone taking irbesartan for high blood pressure?
    ive just started taking it a few days ago and wonder how long it takes to put your bp down. my bp is borderline but due to family history and stress of looking after my mother who has dementia doctor agreed to give me something as i dont want to take any risks, first tried ramapril but that didnt bring it down then switched to felopodine but that made me very ill, migraine and sickness, dont want to give beta blocker as my pulse is relatively low as im quite fit. now have given me irbesartan, no side effects but its not done anything yet as far as i can see when i take bp reading. it says on instructions 4-6 wks for max effect but i wonder when it should start working. anyone know/have experience.
    Heart Doc
    Irbesartan is a great antihypertensive; your doctor has made a good choice.

    I wouldn't be in a major rush to try and lower your BP too quickly. It is only very rarely that we feel the need to do that (and usually in the hospital setting). It is much more appropriate to gently and gradually increase the dose as needed. So that means that if you are monitoring your own BP you might not see a huge difference day-to-day.

    I would suggest first of all that you possibly stop monitoring your BP as frequently. That may in fact make you more anxious and you'll create your own "white coat" effect. If you really want, check it daily (at the same time). If your BP is persistantly above 150/100 by 2 weeks then I would increase your dose (although realistically you could wait 4 weeks).

    What you don't want to do is push the dose to the maximum too quickly and get side-effects you don't need or drop your BP too quickly. Your body has got used to having a slightly raised BP for a while so it won't like a sudden reduction.....a gentle approach always works best (for most things in life!).

    You can worry a bit less now you are on such a good drug. It will certainly help in the long-run.
    macro
    what other generic brand names are equivalent to Aprovel (irbesartan)?
    medication for hypertension
    minty359
    How does it work?

    Aprovel tablets contain the active ingredient irbesartan, which is a type of medicine called an angiotensin II receptor antagonist. It works by preventing the action of a hormone in the body called angiotensin II.

    Angiotensin II normally acts on special receptors in the body, with two main results. Firstly, it causes the peripheral blood vessels to narrow, and secondly, it stimulates the production of another hormone called aldosterone. Aldosterone causes salt and water to be retained by the kidneys, which increases the volume of fluid in the blood vessels.

    Irbesartan blocks the receptors that angiotensin II acts on, and so prevents its actions. The main result of this is that the peripheral blood vessels are allowed to widen, which means that there is more space and less resistance in these blood vessels. This lowers the pressure inside the blood vessels.

    Blocking the actions of angiotensin II also reduces the action of aldosterone on the kidneys. The result of this is an increase in the amount of fluid removed from the blood by the kidneys. This decreases the amount of fluid in the blood vessels, which also lessens the resistance and pressure in the blood vessels.

    The combined overall effect of these changes is to lower the blood pressure.

    What is it used for?

    High blood pressure with no known cause (essential hypertension)

    Kidney disease in people with type 2 diabetes and high blood pressure

    Warning!

    Dizziness and weariness may occasionally occur during treatment with blood pressure lowering medicines. If you are affected, caution is required when driving or operating machinery.

    People with decreased kidney function should have regular blood tests to monitor the levels of potassium and creatinine in their blood while taking this medicine.

    People with heart failure or diabetic kidney disease should have regular blood tests to monitor the level of potassium in their blood while taking this medicine.

    People with high blood pressure caused by high levels of the hormone aldosterone (primary hyperaldosteronism) do not generally respond to this type of blood pressure lowering medicine, and it is not recommended for these people.

    The safety and efficacy of this medicine in children has not been studied by the manufacturer.

    Use with caution in

    Elderly people over 75 years of age

    Decreased kidney function

    People having haemodialysis for kidney failure

    Narrowing of the artery which supplies blood to the kidneys (renal artery stenosis)

    Heart disease caused by inadequate blood flow to the heart (ischaemic heart disease)

    Heart disease characterised by thickening of the internal heart muscle and a blockage inside the heart (hypertrophic obstructive cardiomyopathy)

    Severe heart failure

    Heart valve disease (mitral valve stenosis)

    Narrowing of the main artery of the body (aortic stenosis)

    People with low fluid volume or salt levels in the body, eg due to diuretic therapy, low-sodium diet, diarrhoea or vomiting

    Not to be used in

    Second and third trimesters of pregnancy

    Breastfeeding

    Rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption (Aprovel tablets contain lactose)

    This medicine should not be used if you are allergic to one or any of its ingredients. Please inform your doctor or pharmacist if you have previously experienced such an allergy.

    If you feel you have experienced an allergic reaction, stop using this medicine and inform your doctor or pharmacist immediately.

    Pregnancy and Breastfeeding

    Certain medicines should not be used during pregnancy or breastfeeding. However, other medicines may be safely used in pregnancy or breastfeeding providing the benefits to the mother outweigh the risks to the unborn baby. Always inform your doctor if you are pregnant or planning a pregnancy, before using any medicine.

    This medicine should not be used in pregnancy, particularly in the second and third trimesters, as it may affect the growth and development of the foetus or have adverse effects on foetal tissues. Seek medical advice from your doctor.

    It is not known if irbesartan passes into breast milk. For this reason, the manufacturer states that it should not be used during breastfeeding. Seek medical advice from your doctor.

    Side effects

    Medicines and their possible side effects can affect individual people in different ways. The following are some of the side effects that are known to be associated with this medicine. Because a side effect is stated here, it does not mean that all people using this medicine will experience that or any side effect.

    Dizziness

    Nausea and vomiting

    Fatigue

    A drop in blood pressure that occurs when going from lying down to sitting or standing, which results in dizziness and lightheadedness (postural hypotension)

    Pain in muscles or bones (musculoskeletal pain)

    Diarrhoea

    Indigestion (dyspepsia)

    Increased heart rate (tachycardia)

    Flushing

    Cough

    High blood potassium level (hyperkalaemia)

    Chest pain

    Sexual problems

    Allergic reactions such as itchy, blistering skin rash (urticaria) or swelling of the lips, tongue and throat (angioedema)

    Decreased kidney function

    Headache

    Sensation of ringing or other noise in the ears (tinnitus)

    Muscle cramps

    Abnormal liver function

    The side effects listed above may not include all of the side effects reported by the drug's manufacturer.

    For more information about any other possible risks associated with this medicine, please read the information provided with the medicine or consult your doctor or pharmacist.

    How can this medicine affect other medicines?

    It is important to tell your doctor or pharmacist what medicines you are already taking, including those bought without a prescription and herbal medicines, before you start treatment with this medicine. Similarly, check with your doctor or pharmacist before taking any new medicines while taking this one, to ensure that the combination is safe.

    Irbesartan may enhance the effect of other medicines that decrease blood pressure. In particular, people taking diuretic medicines, eg furosemide, may have a large drop in blood pressure with the first dose. Since this may cause dizziness or fainting, if you are taking a diuretic medicine your doctor may reduce its dose or ask you to stop taking it two to three days before starting irbesartan. This is to prevent your blood pressure from dropping too low.

    This medicine may increase the blood level of the medicine lithium, and it is therefore not recommended for people taking lithium. If your doctor feels the combination is necessary, your lithium level should be closely monitored.

    There may be a risk of raised blood potassium levels (hyperkalaemia) if this medicine is taken with any of the following, hence these are not recommended for use in combination with this medicine:

    potassium-sparing diuretics (eg spironolactone, triamterene, amiloride)

    potassium supplements

    potassium-containing salt substitutes

    other medicines that can increase blood potassium levels, eg heparin.

    Non-steroidal anti-inflammatory drugs (NSAIDs, eg indometacin) may reduce the blood pressure lowering effect of irbesartan. They may also increase the risk of raised blood potassium and kidney problems when used in combination with irbesartan. NSAIDs should be used with caution in people taking irbesartan, particularly elderly people, and your doctor may want to monitor your kidney function.

    Other medicines containing the same active ingredient

    There are currently no other medicines available in the UK that contain irbesartan as the sole active ingredient.

    Medication for High Blood Pressure

    This leaflet is about drugs that are used to treat high blood pressure. A separate leaflet called 'High Blood Pressure' gives more general information about high blood pressure, lifestyle changes that you can do to lower blood pressure, and the reasons why medication is advised to lower blood pressure in some cases.

    What is the aim of treatment?

    The usual target is to reduce blood pressure to below 140/85.

    In some cases, the target is to get it below 130/80 mmHg. For example, if you have diabetes, a cardiovascular disease such as a stroke or heart disease, or if you have certain kidney diseases.

    Which drugs are used to lower blood pressure?

    There are five main classes of drugs that are used to lower blood pressure. There are various types and brands of drug in each class. The following gives a brief overview of each of the classes. However, for detailed information about your own medication you should read the leaflet that comes inside the drug packet.

    Angiotensin-converting enzyme (ACE) inhibitors

    These drugs work by reducing the amount of a chemical that you make in your bloodstream called angiotensin II. This chemical tends to constrict (narrow) blood vessels. Therefore, less of this chemical causes the blood vessels to relax and widen, and so the pressure of blood within the blood vessels is reduced.

    There are various types and brands of ACE inhibitors. For example, captopril, cilazapril, enalapril, fisinopril, lisinopril, perindopril, quinapril, ramipril, and trandolapril. An ACE inhibitor is particularly useful if you also have heart failure or diabetes. ACE inhibitors should not be taken by people with certain types of kidney problems, people with some types of artery problems, and if you are pregnant. You will need a blood test before starting an ACE inhibitor, and within a week after starting it, and one week after any increase in dose. Then, a yearly blood test is usual.

    Angiotensin Receptor Blockers

    These drugs are sometimes called angiotension II receptor antagonists. There are various types and brands. For example, candesartan, eprosartan, irbesartan, losartan, olmesartan, telmisartan and valsartan. They work by blocking the effect of angiotensin II on the blood vessel walls. So, they have a similar effect to ACE inhibitors (described above).

    Calcium-channel blockers

    These drugs affect the way calcium is used in the blood vessels and heart muscle. This has a relaxing effect on the blood vessels. Again, there are various types and brands. For example, amlodipine, diltiazem, felodipine, isradipine, lacidipine, lercanidipine, nicardipine, nifedipine, nisoldipine, and verapamil. Calcium-channel blockers can also be used to treat angina.

    Diuretics ('water tablets')

    The most commonly used diuretic to treat high blood pressure in the UK is called bendroflumethiazide (bendrofluazide) - but there are others. For example, chlorothiazide, chlorthalidone, cyclopenthiazide, hydrochlorothiazide, and indapamide. Diuretics work by increasing the amount of salt and fluid that you pass out in your urine. This has some effect on reducing the fluid in the circulation which reduces blood pressure. They may also have a 'relaxing' effect on the blood vessels which reduces the pressure within the blood vessels. Only a low dose of a diuretic is needed to treat high blood pressure. Therefore, you will not notice much diuretic effect (you will not pass much extra urine).

    Beta-blockers

    Again, there are various types and brands. For example, acebutolol, atenolol, bisoprolol, metoprolol, oxprenolol, pindolol, propanaolol, sotalol, and timolol. They work by slowing the heart rate, and reducing the force of the heart. These actions lower the blood pressure. Beta-blockers are also commonly used to treat angina, and some other conditions. You should not take a beta-blocker if you have asthma, chronic obstructive pulmonary disease (COPD), or certain types of heart or blood vessel problems.
    Matt
    which is better for hypertension termisartan(micardes) or Irbesartan(approvel)?
    Previous...
    They are in the same class.

    It is just how it works with the person's physiology.

    Usually Micardis is used more often.
    Bren
    anyone taking irbesartan(approvel) for high blood pressure?
    have u noticed any problem keeping yr weight under control. since taking it i have found i have put on about a stone in weight i seem to have an insatiable appetite and find it hard to keep to a diet . im loathe to ask my doc to change the medication as its working at last with relatively little side effect - in the winter i suffered badly with cold hands and feet but now the weather is warmer i dont have that problem and the 24 hr bp monitor test said that its controlling my bp well. im tended to let sleeping dogs lie but if its this causing my weight gain then i have to think again as being overweight doenst help if u have bp problems.
    ajmill19...
    This depends. I should first state that weight gain is not a side effect reported for irbesartan or any of the other -sartan drugs (ARBs).

    A stone is 14 pounds and if you gained that in 2 weeks it could be a fairly serious issue that you'd want to talk to you doctor about. It sounds like you've been on this ARB for at least 6 months now, though, so you're not going to just magically normalize "in a few weeks".

    Weight gain can be caused by a lot of things. If you were on a powerful diuretic in the past (e.g. furosemide) to control you blood pressure, and the doctor took you off it, several pounds of that weight could just be water, as you've readjusted to the new medication.

    At this point, you're probably on more than just one medication for your blood pressure, or you might have some other chronic disease state (like diabetes). Sometimes what we *think* is due to a change in just one drug is really a combination of effects from other drugs as well, even if you've been doing well on them in the past.

    Without more information, I can't make any more detailed guesses. But it's certainly something to talk to your doctor about if you're concerned.

    Added info:

    Your observations are exactly what you need to bring to your doctor's attention. A 14lb weight gain over a year is about 1-2lbs a month and this is nothing to be greatly concerned about. Over a year, there can be a lot of small changes to your lifestyle that you may not notice. There are also a lot of hormonal changes that happen to a woman of your age that could be contributing to weight gain. Have you had your HbA1C checked for signs of early diabetes? That's yet another reason for unexplained weight gain, and isn't just limited to "at risk" populations.

    Point being, there are many potential causes for gradual sustained weight gain. If your blood pressure, liver, kidneys, and blood glucose all test well, then your next step would be to talk to a nutritionist and see if perhaps some small changes can nudge you in the other direction. Good luck, and don't let your GP off the hook, that's what he's there for!
    cuckoo's got nothin to lose
    What does "mane"(in latin, medical, pharmacy field) mean?
    From a prescription, for example, "Irbesartan 300mg mane"

    What does this really mean?
    proud to be an indian-sri ravali
    it is redirected from Cras Mane (Latin: tomorrow morning;used in medical prescription instructions)

    Naomi M
    Does anyone know anything about the stroke treatment called ASTART - Accute Stroke Treatment?
    Do you know anyone who has had this treatment? ASTART (Accute Stroke Treatment with Atorvastatin and Irbesartan)This treatment is a study and patients are randomly chosen (toss of coin), patients put into 4 groups. 1 group takes Irbesartan Blood pressure tablet and cholesterol tablet Atorvastatin, 2nd group - Irbesartan alone, 3rd Atorvastatin alone 4th group - Placebo (dummy tablet). Staff will not know what treatment patient is on. My father started taking this tonight 26/3/07 and I would really appreciate any information someone may have email me at nymiller78@yahoo.com
    nickname
    Naomi, I haven't heard of it. Have you tired looking up clinical trials on the web? I've somehow gotten to that website and literlly have found hundreds. Have you tried emailing the companies? Good luck hope you get what you need
    angelfir...
    atheromatous aorta? How bad is it?
    Am currently on Irbesartan 150 mg, Norvasc 5 mg and Simvastatin Zocor 20 mg......

    Is an atheromatous aorta condition reversible through medication?
    vascsono
    Atheromatous Aorta means you have some plaque on the aorta. (atherosclerosis=plaque). I do not know how significant your plaque is however.

    It appears you are on anti-hypertensive medications as well as lowering cholesterol meds. That is good. BUT, u need to eat right and exercise. and if you smoke YOU MUST STOP NOW.

    Walk a mile a day each day to build extra vessels in your heart, legs and abdomen. So if there is a significant narrowing, with increased activity, your own body may prevent surgery (by growing bridge vessels around blockages aka collaterals).
    suresh b
    What is the difference between Angiotensin receptor blockers structurally nad functionally?Which ARB is better
    Irbesartan>Telmisartan>Valsartan>Losarta...
    gangadha...
    Please see the web pages for more details on Angiotensin receptor blocker, such as Irbesartan, Telmisartan, Valsartan, and Losartan.

    Consult a cardiologist.
    ezmareld...
    Medication of Aprovel and Mirtazapine!?
    My mum takes Aprovel (Irbesartan) for high blood pressure and Mirtazapine for depression but she complains of light headedness all the time. The doctor has switched her to a different blood pressure tablet called Karveside ,but to no avail. She has been on the medication for months and it is affecting her quality of life. Her depression has gone but the 'light headedness' affects her and she does not like going out much. Any physicians out there or anyone with a similar experience. Help! Thanks!
    The Rugby Player
    I have got a similar problem.

    I have changed all types of medications and now I am on 9 tablets a day

    My wife is pushing me hard but I am grateful for the attention and whatever little exercise she pushes me to do.
    joan1214
    my mom 's having high blood pressure/hypertension for almost 20 years, n recently she's attacked by 'stroke'!!
    now, she's recovering from stroke very 'slowly'!!some medications were prescribed:-->piracetam(Nootropil), Nifedipine(Adalat), irbesartan(Approvel), Gliclzide(Diamacron MR), and glucophage.

    may i know d uses of each medicine prescibed??n according to d doctor, stroke cannot be recovering 100%, is tat true??after d stroke, right part of her limbs are weak (cuz there's hemorrhage in d brain as one of d blood vessel burst)..she's been doing physiotherapy, but d leg mscle's still very weak..wat can she do to walk like a normal people??is tat possible??some ppl said, d main reason tat she can't walk properly is due to the brain damage, not the muscle problem..may i know the correct answer?? will the brain damage recover perfectly..or it won't recover, or it'll recover slowly??when she try to walk, she felt atching, and fatigue on d leg, should she continue to practice walking?n her eyesight is poor n blur, why??

    does d medication sufficient to let her relapse as much as possible?
    bettyboo...
    piracetam will help with the bleeding in the brain, adalat is for her blood pressure, irbesartan is also for her blood pressure, diamacron MR is for high blood pressure and glucophage is for diabetes. Recovery for a stroke is not 100%. Her limbs will be weak and she really needs the physical therapy. Part of the brain has been damaged, and will need to be retrained to work the muscles again. It will be a long process over a period of months. She will feel tired, that is to be expected. She will also ache and have pains. Ask the dr. if it is ok to take tylenol for her pain. She should continue to practice walking. If her eysight is poor and it didn't use to be, then the stroke affected her vision also, due to the brain injury, or possible stroke in the eye. Hopefully, and more than likely, the medication she is on will keep her from having a relapse. Also you need to let her do as much as possible for herself. You can show her how and then encourage her to do it herself, as much as possible and reasonable.