Sunday, April 28, 2013

DOXAZOSIN


Doxazosin mesylate, a quinazoline compound sold by Pfizer under the brand names Cardura and Carduran, is an α1-selective alpha blocker used to treat high blood pressure and urinary retention associated with benign prostatic hyperplasia (BPH).
On February 22, 2005, the US FDA approved a sustained release form of doxazosin, to be marketed as Cardura XL.
It is an alpha-1 adrenergic receptor blocker that inhibits the binding of norepinephrine (released from sympathetic nerve terminals) to the alpha-1 receptors on the membrane of vascular smooth muscle cells. The primary effect of this inhibition is relaxed vascular smooth muscle tone (vasodilation), which decreases peripheral vascular resistance, leading to decreased blood pressure.
Doxazosin and similar medications like prazosin have been found to help reduce the intensity of and/or stop posttraumatic stress disorder night terrors and nightmares. The full reasoning of this effect is not understood.
In Egypt, tablet formulation sold as Duracin produced by Biopharm group for research and the drug industry, Dosin by Eipico and Doxazocine by Multi-Apex.

(RS)-2-{4-[(2,3-Dihydro-1,4-benzodioxin-2-yl)carbonyl]piperazin-1-yl}-6,7-dimethoxyquinazolin-4-amine


EFFICACY
In March 2000, the ALLHAT study stopped its arm of the trial looking at alpha blockers, because doxazosin was less effective than a simple diuretic, and because patients on doxazosin had a 25% higher rate of cardiovascular disease and twice the rate of congestive heart failure as patients on diuretics. Pfizer, aware of the results before publication, launched a marketing campaign in early 2000, and sales were largely unaffected, despite the dangers highlighted by the study. Doxazosin shows potential for treatment of benign prostatic hyperplasia and erectile dysfunction.
Doxazosin has also shown some efficacy in treating chronic epididymitis.



INDICATION AND DOSAGE
Hypertension
Adult: As mesilate: Initially, 1 mg at bedtime increased after 1-2 wk according to response. Maintenance: 4 mg once daily. Max: 16 mg daily.

Benign prostatic hyperplasia
Adult: As mesilate: Initially, 1 mg once daily at bedtime increased after 1-2 wk; monitor BP after 2-6 hr. Maintenance: 2-4 mg daily. Max: 8 mg daily



Contraindications Known hypersensitivity to quinazolines.

Special Precautions Renal or hepatic impairment. Prostatic carcinoma should be ruled out before starting therapy. Orthostatic hypotension may occur at the initiation of therapy or when there is dose increase. Avoid driving or performing hazardous tasks for 24 hr after starting therapy or dose changes. Pregnancy and lactation.

Adverse Drug Reactions Chest pain, fatigue, headache, influenza-like symptoms, pain, hypotension, palpitation, abdominal pain, diarrhoea, nausea, oedema, dizziness, dry mouth, somnolence, dyspnoea, respiratory disorders, vision abnormalities, impotence, urinary tract infection, increased sweating, anxiety, insomnia. Vertigo, orthostatic hypotension, arrhythmia, hypotension, arthralgia/arthritis, muscle weakness, myalgia, kinetic disorders, ataxia, hypertonia, muscle cramps, flushing, tinnitus, sexual dysfunction, rhinitis, epistaxis, polyuria, urinary incontinence, fatigue/malaise, face oedema.



BRAND - DOXACARD

DILTIAZEM


Diltiazem is a nondihydropyridine (non-DHP) member of the class of drugs known as calcium channel blockers, used in the treatment of hypertension, angina pectoris, and some types of arrhythmia.
It is also an effective preventive medication for migraine. It is a class 3 antianginal drug, and a class IV antiarrhythmic. It is a common adulterant of cocaine seized in the UK, and has been found to reduce cocaine cravings in rats, indicating it may prolong the "high" (see below). It incites minimal reflex sympathetic changes. It is based upon a 1,4-thiazepine ring.
Diltiazem is metabolized by and acts as an inhibitor of the CYP3A4 enzyme.

cis-(+)-[2-(2-dimethylaminoethyl)-5-(4-methoxyphenyl)
-3-oxo-6-thia-2-azabicyclo[5.4.0]undeca-7,9,
11-trien-4-yl]ethanoate



MECHANISM

Diltiazem is a potent vasodilator, increasing blood flow and variably decreasing the heart rate via strong depression of A-V node conduction. Its pharmacological activity is somewhat similar to verapamil.
It is a potent vasodilator of coronary and peripheral vessels, which reduces peripheral resistance and afterload.
Because of its negative inotropic effect, diltiazem causes a modest decrease in heart muscle contractility and reduces myocardium oxygen consumption. Its negative chronotropic effect results in a modest lowering of heart rate, due to slowing of the sinoatrial node. It results in reduced myocardium oxygen consumption.
Because of its negative dromotropic effect, conduction through the AV (atrioventricular) node is slowed, which increases the time needed for each beat. This results in reduced myocardium oxygen consumption.



INDICATIONS

The drug is indicated for angina:
Stable angina (exercise-induced) – diltiazem increases coronary blood flow and decreases myocardial oxygen consumption, secondary to decreased peripheral resistance, heart rate, and contractility.
Variant angina – it is effective owing to its direct effects on coronary dilation.
Unstable angina (preinfarction, crescendo) – diltiazem may be particularly effective if the underlying mechanism is vasospasm.
For supraventricular tachycardias, diltiazem appears to be as effective as verapamil in treating re-entrant supraventricular tachycardia.
Atrial fibrillation or atrial flutter PSVT is another indication. The initial bolus should be 0.25mg/kg, intravenous (IV).
Because of its vasodilatory effects, diltiazem is useful for treating hypertension. Calcium channel blockers are well tolerated, and especially effective in treating low-renin hypertension.



DOSE
The dose of diltiazem in supraventricular tachycardias is 0.25 mg/kg, slow IV push. Most commonly, a 20-mg IV dose is given to the average-sized patient.


DRUG INTERACTIONS
Beta-blockers
Intravenous diltiazem should be used with caution with beta-blockers because, while the combination is most therapeutically beneficial, there are rare instances of dysrhythmia and AV node block.
Quinidine
Quinidine should not be used concurrently with calcium channel blockers because of reduced clearance of both drugs and potential pharmacodynamic effects at the SA and AV nodes.
Miscellaneous
Diltiazem and verapamil inhibit hepatic cytochromes CYP3A4, CYP2C9 and CYP2D6, possibly resulting in drug interactions

BRAND NAMES
Progor, Altiazem, Cardizem, Cartia XT, Tiazac, Tiazac XC, Tiamate, Taztia XT, Tildiem particularly in Europe, Adizem
Viazem, Dilatam, Dilzem, Angiozem, Dilatem, Dilcardia, Diltelan, Diltime, Diltiact in India, Dyalec, Filazem, Tildiem,
Vasmulax, Vasocardol in Australia, Zandil, Zemtrial, Angizem CD, Angizem, Dilcontin Xl, Dilt-CD, Dilt-XR, Corzem in Jordan




Saturday, April 27, 2013

CLONIDINE


 Clonidine is a sympatholytic medication used to treat high blood pressure, ADHD, anxiety/panic disorder, and certain pain conditions. It is classified as a centrally acting α2 adrenergic agonist. An alternative hypothesis that has been proposed is that clonidine acts centrally as an imidazoline receptor agonist.

N-(2,6-dichlorophenyl)-4,5-dihydro-1H-imidazol-2-amine


USE

Clonidine has been investigated and prescribed first as an antihypertensive drug in the 1950s. It has found new uses later, including treatment of some types of neuropathic pain, opioid detoxification, sleep hyperhidrosis, and as veterinary anaesthetic drug. Clonidine is used to treat anxiety and panic disorder. It is also FDA approved to treat ADHD in an extended release form. It is becoming a more accepted treatment for insomnia, as well as for relief of menopausal symptoms.

Clonidine is increasingly used in conjunction with stimulants to treat attention-deficit hyperactivity disorder (ADHD), for which it is administered in late afternoon or evening for sleep, and because it sometimes helps moderate ADHD-associated impulsive and oppositional behavior, and may reduce tics, a problem in which a part of the body moves repeatedly and suddenly. Clonidine can be used in the treatment of Tourette syndrome (specifically for tics). Clonidine along with methylphenidate has been studied for treatment of ADHD. In 2010, the Food and Drug Administration approved the use of clonidine either as an adjunct to traditional stimulant therapy or as a monotherapy in the treatment of attention deficit hyperactivity disorder (ADHD).

Clonidine may be used to ease withdrawal symptoms associated with the long-term use of narcotics, alcohol and nicotine (smoking). It can alleviate opioid withdrawal symptoms by reducing the sympathetic nervous system response such as tachycardia and hypertension, as well as reducing sweating, hot and cold flushes, and general restlessness.The sedation effect is also useful although its side effects can include insomnia, thus exacerbating an already common feature of opioid withdrawal.
For some of the above reasons, clonidine is also used in some cases as an active placebo for narcotic analgesics in clinical trials and other lab experiments on morphine and its derivatives and mimics.

Clonidine can be used for migraine headaches and hot flushes associated with menopause.

Clonidine also has several off-label uses, and has been prescribed to treat psychiatric disorders including stress, sleep disorders, and hyperarousal caused by post-traumatic stress disorder, borderline personality disorder, and other anxiety disorders. Clonidine is also a mild sedative, and can be used as premedication before surgery or procedures. Its epidural use for pain during heart attack, postoperative and intractable pain has also been studied extensively.Clonidine has also been suggested as a treatment for rare instances of dexmedetomidine withdrawal.
Clonidine has also been found to prolong the effects of analgesia when used together with a local anesthetic such as ropivacaine or levobupivacaine.



MECHANISM OF ACTION
Clonidine treats high blood pressure by stimulating α2 receptors in the brain, which decreases cardiac output and peripheral vascular resistance, lowering blood pressure. It has specificity towards the presynaptic α2 receptors in the vasomotor center in the brainstem. This binding decreases presynaptic calcium levels, and inhibits the release of norepinephrine (NE). The net effect is a decrease in sympathetic tone.
It has also been proposed that the antihypertensive effect of clonidine is due to agonism on the I1-receptor (imidazoline receptor), which mediates the sympatho-inhibitory actions of imidazolines to lower blood pressure.

PREPERATION
Clonidine is typically available as tablets (Catapres, Dixarit), extended-release tablets (Kapvay), as a transdermal patch (Catapres-TTS), or as an injectable form to be given i.m., i.v. or epidurally - directly to the central nervous system.


BRAND -  CATAPRESS

Thursday, April 25, 2013

HEART HEALTHY FOOD 1




Heart disease is a major health concern, killing around half a million people or more each year in the United States alone. Exercise and portion control are important in preventing or controlling heart disease, but what you eat, not just how much you eat, makes a big difference too. There are many fruits and vegetables that are good for your heart. You should be eating more of them more often.

Fruits and vegetables are more than just good sources of vitamins and minerals; they are low in calories, rich in dietary fiber, full of antioxidants, low in saturated fat, and naturally cholesterol free.
Antioxidants keep free radicals from damaging blood vessels and the heart. Antioxidants also keep cholesterol and blood platelets from becoming sticky, preventing dangerous clots.
Dietary fiber cannot be absorbed or used by the body, but is far more valuable than this makes it sound. Fiber slows absorption of sugars. Repeated sugar spikes can damage the lining of arteries, leading to hardening and plaque buildup. Fiber also binds to cholesterol and fat during digestion, safely moving it out of the body. In much the same way, fiber removes toxins, waste, and pollutants that can also cause damage to cells, arteries, and muscles like the heart. Fiber also helps lower blood pressure.

Acorn Squash – This winter squash is an excellent source of vitamin A that prevents the oxidization of cholesterol that can lead to plaque buildup. They are also a good source of fiber and vitamin C, a powerful antioxidant.

Almonds – These nuts are rich in monounsaturated fats that actually protect the heart. They are also a good source of fiber and antioxidants.

Asparagus – Asparagus is packed with fiber, folic acid, vitamin C, and potassium. Potassium plays a key part in regulating heart function and controlling blood pressure. Folic acid and vitamin C help prevent heart disease.

Avocado – This green savory fruit is a heart health powerhouse, filled with fiber, B vitamins, vitamin C, good fats, and potassium.

Beans – Black or kidney, beans are an excellent source of fiber, healthy fats, and B vitamins.

Blueberries – These small berries pack a lot of antioxidant punch, containing compounds similar to the heart healthy ones found in grapes and wine. Paired with fiber, these antioxidants help control cholesterol levels and keep plaque at bay.

Broccoli – This flowering vegetable contains sulforaphane, a compound that triggers defense mechanisms that reduce inflammation and protect the arteries from damage and disease. Broccoli is a rich source of heart healthy fiber, vitamin A, and vitamin C. Broccoli is also one of the few plants that contain co-enzyme Q10 which plays a crucial role in muscle health and strength, including the heart.

Brown Rice – White rice has been stripped of the bran along with many vitamins and minerals. Brown rice, on the other hand, is rich in fiber and powerful antioxidants. Brown rice also contains special compounds called lignans that fight heart disease.

Cantaloupe – This fresh summer melon contains fiber, potassium, vitamin C, and vitamin A, all of which protect the heart.

Carrots – Rich in beta carotene which is converted to vitamin A, carrots prevent the oxidization of cholesterol. They are also rich in fiber, vitamin C, and potassium.

Chia – These seeds have an abundance of healthy fat and fiber, along with healthy protein. Chia supplies all the heart healthy benefits of flax without the concerns surrounding phytoestrogens.

Dark Chocolate – Dark chocolate contains compounds called flavanols, which have antioxidant and anti-inflammatory properties. Dark chocolate also balances blood sugar and cholesterol levels.

Oatmeal – Filled with fiber, potassium, and healthy fats, oatmeal combats heart disease, lowers cholesterol, and brings down blood pressure. Oatmeal also contains some unique and powerful antioxidants.

Oranges – Oranges and grapefruit contain flavanones, powerful compounds that can drastically lower bad cholesterol and raise good cholesterol levels. They are also rich in antioxidants, vitamin C, and B vitamins.

Papaya – Papaya is exceptionally rich in vitamin C, vitamin A, folic acid, potassium, and fiber. They also have anti-inflammatory properties.

Red Bell Pepper – Bell peppers of any color contain large amounts of vitamin A and vitamin C, but red bell peppers supply the most. They are also rich in B vitamins and contain some capsaicin that helps with blood flow and cholesterol.

Grapes – Grapes contain a powerful antioxidant in their skins called resveratrol along with other antioxidants and anti-inflammatories. These improve blood pressure, cholesterol, and prevent plaque.

Spinach – Another plant that contains co-enzyme Q10, which supplies energy to muscle cells and may also lower cholesterol levels. Spinach is also rich in potassium for blood pressure, fiber to continue lowering cholesterol and remove toxins, folic acid, and many antioxidants.

Sweet Potato – Much better for you than their white counterparts, sweet potatoes contain potassium, fiber, vitamin A, and vitamin C.

Tomatoes – Lycopene, the pigment that gives tomatoes their bright red color, is a mighty antioxidant that can lower cholesterol and protect the heart and arteries from free radical damage. They are also rich in vitamin C, vitamin A, and potassium.

Walnuts – Like almonds, walnuts are rich in monounsaturated fats that actually protect the heart and a good source of fiber and antioxidants.

Wednesday, April 24, 2013

CHLORTHALIDONE


Chlortalidone  or chlorthalidone (USAN) is a diuretic drug used to treat hypertension, originally marketed as Hygroton in the USA. It is described as a thiazide diuretic (or, rather, a thiazide-like diuretic because it acts similarly to the thiazides but does not contain the benzothiadiazine molecular structure). Compared with other medications of the thiazide class, chlortalidone has the longest duration of action but a similar diuretic effect at maximal therapeutic doses. It is often used in the management of hypertension and edema.
Unlike loop diuretics, chlortalidone efficacy is diminished in patients with certain renal diseases (e.g. chronic renal disease). A clinical trial  in 2002 compared chlortalidone to doxazosin in the treatment of high-risk hypertensive patients. In this study, only chlortalidone significantly reduced the risk of combined cardiovascular disease events, especially heart failure, when compared with drugs such as doxazosin. Chlortalidone was approved by the FDA in 1960. The ALLHAT study conclusions showed that there was no significant difference in all-cause mortality, fatal heart disease, or non-fatal myocardial infarction when chlortalidone was compared with lisinopril or amlodipine but did show decrease rates of heart failure after 6 years when compared with amlodipine and decreased rates of cerebrovascular disease after 6 years when compared with lisinopril leading the study conclusions to say that thiazide-type diuretics are preferred first-step in antihypertensive therapy.


(RS)-2-chloro-5-(1-hydroxy-3-oxo-2,3-dihydro-1H-isoindol-1-yl)benzene-1-sulfonamide

Mechanism of action

Chlortalidone increases the excretion of sodium, chloride, and water into the renal lumen by inhibiting sodium ion transport across the renal tubular epithelium. Its primary site of action is in the cortical diluting segment of the ascending limb of the loop of Henle. Thiazides and related compounds also decrease the glomerular filtration rate, which further reduces the drug's efficacy in patients with renal impairment (e.g. renal insufficiency). By increasing the delivery of sodium to the distal renal tubule, chlortalidone indirectly increases potassium excretion via the sodium-potassium exchange mechanism (i.e. apical ROMK/Na channels coupled with basolateral NKATPases). This can result in hypokalemia and hypochloremia as well as a mild metabolic alkalosis; however, the diuretic efficacy of chlortalidone is not affected by the acid-base balance of the patient being treated.
Initially, diuretics lower blood pressure by decreasing cardiac output and reducing plasma and extracellular fluid volume. Eventually, cardiac output returns to normal, and plasma and extracellular fluid volume return to slightly less than normal, but a reduction in peripheral vascular resistance is maintained, thus resulting in an overall lower blood pressure. The reduction in intravascular volume induces an elevation in plasma renin activity and aldosterone secretion, further contributing to the potassium loss associated with thiazide diuretic therapy.

Other use
Chlorthalidone may also be used to treat patients with diabetes insipidus and certain electrolyte disturbances and to prevent kidney stones in patients with high levels of calcium in their blood. Talk to your doctor about the possible risks of using this medicine for your condition.


Before taking chlorthalidone,
tell your doctor and pharmacist if you are allergic to chlorthalidone, sulfa drugs, or any other drugs.
tell your doctor and pharmacist what prescription and nonprescription medications you are taking, especially other medicines for high blood pressure, anti-inflammatory medications such as ibuprofen (Motrin, Nuprin) or naproxen (Aleve), corticosteroids (e.g., prednisone), lithium (Eskalith, Lithobid), medications for diabetes, probenecid (Benemid), and vitamins. If you also are taking cholestyramine or colestipol, take it at least 1 hour after chlorthalidone.
tell your doctor if you have or have ever had diabetes, gout, or kidney, liver, thyroid, or parathyroid disease.
tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant while taking chlorthalidone, call your doctor immediately.
if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking chlorthalidone.
you should know that this drug may make you drowsy. Do not drive a car or operate machinery until you know how this drug affects you.
remember that alcohol can add to the drowsiness caused by this drug.
plan to avoid unnecessary or prolonged exposure to sunlight and to wear protective clothing, sunglasses, and sunscreen. Chlorthalidone may make your skin sensitive to sunlight.


Usual Adult Dose for Edema
Initial dose: 50-100 mg orally once a day.
Maintenance dose: 25-100 mg once a day or
50-200 mg every other day.

Usual Adult Dose for Hypertension
Initial dose: 25 mg orally once a day (15 mg for Thalitone).
Maintenance dose: 25-100 mg once a day (15-50 mg for Thalitone).

Renal Dose Adjustments
Chlorthalidone is not expected to be filtered into the renal tubule (its site of action) when the glomerular filtration rate is less than 10 mL/min.

Dose Adjustments
Dosage adjustments are recommended to be made no more frequently than weekly. Patients with liver disease or renal dysfunction should have dosage adjustments made cautiously.



Tuesday, April 23, 2013

Celiprolol


Celiprolol  is a medication in the class of beta blockers, used in the treatment of high blood pressure. It has a unique pharmacology: it is a selective β1 receptor antagonist, but a β2 receptor partial agonist. It is also a weak α2 receptor antagonist.
A recent clinical trial has suggested a use for this medication in the prevention of vascular complications of a rare inherited disease called vascular Ehlers–Danlos syndrome. This study demonstrated decreased incidence of arterial rupture or dissection (a specific type of arterial rupture in which the layers of the vessel separate prior to complete failure of the artery wall)


Brand names -  Cardem, Selectol, Celipres, Celipro, Celol, Cordiax, Dilanorm

(RS)-N'-{3-acetyl-4-[3-(tert-butylamino)-2-hydroxypropoxy]phenyl}-N,N-diethylurea

Before taking celiprolol

Some medicines are not suitable for people with certain conditions, and sometimes a medicine may only be used if extra care is taken. For these reasons, before you start taking celiprolol it is important that your doctor or pharmacist knows:

If you are pregnant, trying for a baby or breast-feeding.
If you have liver or kidney problems.
If you have low blood pressure or poor circulation.
If you have asthma or breathing difficulties.
If you have sugar diabetes.
If you have psoriasis (a skin problem).
If you have myasthenia gravis (a condition causing muscle weakness).
If you have been told you have a slow heartbeat or heart block (a slow and irregular heartbeat).
If you have been told you have Prinzmetal's angina (chest pain caused by spasms of the heart's blood vessels).
If you have phaeochromocytoma (a tumour on your adrenal gland).
If you are taking other medicines, including those available to buy without a prescription, herbal and complementary medicines.
If you have ever had an allergic reaction to a medicine, or if you have ever had any other severe allergic reaction.



How to take celiprolol


Before you start this treatment, read the manufacturer's printed information leaflet from inside the pack. The leaflet will give you more information about celiprolol and a full list of side-effects which you may experience from taking it.
Take celiprolol exactly as your doctor has told you. There are two strengths of tablet - 200 mg and 400 mg. It is usual to start by taking one 200 mg tablet daily, although your doctor may later increase this to the 400 mg strength tablet. You should take the tablet first thing in the morning, preferably 'on an empty stomach'. This means that you should take it at least 30 minutes before breakfast or wait until two hours afterwards. Swallow the tablet with a drink of water.
If you forget to take a dose, take it when you remember. (If possible, remember to take it half an hour before a meal, or two hours after a meal). If you do not remember until the following day, skip the missed dose. Do not take two doses together to make up for a forgotten dose.

Getting the most from your treatment

Try to keep your regular appointments with your doctor. This is so your doctor can check on your progress.
It is very important to follow any dietary and lifestyle advice that you may have been given by your doctor, such as eating a healthy diet, not smoking, and taking regular exercise.
If you drink alcohol, ask your doctor for advice about taking celiprolol and alcohol. Alcohol will add to the blood pressure lowering effect of celiprolol and so may not be recommended for you.
If you have diabetes, celiprolol may block the symptoms of low blood sugar. Your doctor will be able to advise you about this.
If you are having an operation or dental treatment, tell the person carrying out the treatment that you are taking a beta-blocker.
Treatment with celiprolol is usually long-term so continue to take these tablets unless your doctor tells you to stop. Stopping treatment suddenly can cause problems in some people, so your doctor will probably want you to reduce your dose gradually if this is necessary.
If you buy any medicines, check with a pharmacist that they are suitable for someone with high blood pressure to take. Some medicines (including some cough, cold and flu remedies) may not be.


How to store celiprolol

Keep all medicines out of the reach and sight of children.
Store in a cool, dry place, away from direct heat and light


Taking other medicines

If you are taking more than one medicine they may interact with each other. At times your prescriber may decide to use medicines that interact, in other cases this may not be appropriate.
The decision to use medicines that interact depends on your specific circumstances. Your prescriber may decide to use medicines that interact, if it is believed that the benefits of taking the medicines together outweigh the risks. In such cases, it may be necessary to alter your dose or monitor you more closely.
Tell your prescriber the names of all the medicines that you are taking so that they can consider all possible interactions. This includes all the medicines which have been prescribed by your GP, hospital doctor, dentist, nurse, health visitor, midwife or pharmacist. You must also tell your prescriber about medicines which you have bought over the counter without prescriptions.
The following medicines may interact with Celiprolol hydrochloride:
adrenaline
amiodarone
chlortalidone
clonidine
cyclopropane
diltiazem
disopyramide
ether
floctafenine
hydrochlorothiazide
ibuprofen
indometacin
insulin
mefloquine
nifedipine
quinidine
theophylline
trichloroethylene
verapamil
The following types of medicine may interact with Celiprolol hydrochloride:
anaesthetics
antiarrhythmics
antihypertensives
barbiturates
calcium channel blockers
digitalis glycosides
dihydropyridine derivatives
monoamine oxidase inhibitors
oral antidiabetics
phenothiazines
prostaglandin synthetase inhibitors
sympathomimetics
tricyclic antidepressants






Sunday, April 14, 2013

CARVEDILOL


Carvedilol is a nonselective beta blocker/alpha-1 blocker indicated in the treatment of mild to severe congestive heart failure (CHF). It is marketed under various trade names including Carvil (Zydus Cadila), Coreg (GSK), Dilatrend (Roche), Eucardic (Roche), and Carloc (Cipla) as a generic drug (as of September 5, 2007 in the U.S.), and as a controlled-release formulation, marketed in the US as Coreg CR (GSK). Carvedilol was discovered by Robert R. Ruffolo, Jr. It has had a significant role in the treatment of congestive heart failure.



(±)-[3-(9H-carbazol-4-yloxy)-2-hydroxypropyl][2-(2-methoxyphenoxy)ethyl]amine


USE AND DOSE

Carvedilol is indicated in the management of congestive heart failure (CHF), as an adjunct to conventional treatments (ACE inhibitors and diuretics). The use of carvedilol has been shown to provide additional morbidity and mortality benefits in severe CHF. Carvedilol (Carvil) is available at the following doses 3.125 mg (smallest), followed by 6.25 mg,12.5 mg, and 25 mg white tablets.

Hypertension  -  Oral
Adult: Initially, 12.5 mg once daily increased to 25 mg once daily after 2 days. Alternatively, initial dose of 6.25 mg bid increased to 12.5 mg bid after 1-2 wk, increased further if necessary to 50 mg once daily or in divided doses.
Elderly: 12.5 mg once daily.

Angina pectoris  -  Oral
Adult: Initially, 12.5 mg bid increased to 25 mg bid after 2 days.

Heart failure  -  Oral
Adult: Initially, 3.125 mg bid, doubled to 6.25 mg bid after 2 wk if tolerated, then gradually increased to the max dose the patient can tolerate at intervals of not <2 dose:="" max="" wk.="">85 kg: 50 mg bid; <85 25="" bid.="" kg:="" mg="" p="">
Left ventricular dysfunction post myocardial infarction  - Oral
Adult: Initially: 6.25 mg bid, if tolerated, after 3-10 days, increase to 12.5 mg bid and then to a target dose of 25 mg bid.


PHARMACOLOGY

Carvedilol is both a beta blocker (β1, β2) and alpha blocker (α1):
Norepinephrine stimulates the nerves that control the muscles of the heart by binding to the β1- and β2-adrenergic receptors. Carvedilol blocks the binding to those receptors, which both slows the heart rhythm and reduces the force of the heart's pumping. This lowers blood pressure thus reducing the workload of the heart, which is particularly beneficial in heart failure patients.
Norepinephrine also binds to the α1-adrenergic receptors on blood vessels, causing them to constrict and raise blood pressure. Carvedilol blocks this binding to the α1-adrenergic receptors too, which also lowers blood pressure.
Relative to other beta blockers, carvedilol has minimal inverse agonist activity. This suggests that carvedilol has a reduced negative chronotropic and inotropic effect compared to other beta blockers, which may decrease its potential to worsen symptoms of heart failure. However, to date this theoretical benefit has not been established in clinical trials, and the current version of the ACC/AHA guidelines on congestive heart failure management does not give preference to carvedilol over other beta-blockers.
Carvedilol does also act as FIASMA (functional inhibitor of acid sphingomyelinase).

SIDE EFFECTS - The most common side effects include dizziness, fatigue, hypotension, diarrhea, asthenia, bradycardia, and weight gain

DRUG INTERACTIONS

Epinephrine WITH  carvedilol
Beta-blockers like carvedilol may reduce the effects of epinephrine. If you have been using carvedilol, you may not respond as well to epinephrine when it is given to treat an emergency such as shock or a severe allergic reaction. In addition, the combination may cause severe high blood pressure and reduced heart rate. Your healthcare provider should always be told if you are receiving, or have recently received, beta-blocker therapy. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.

Albuterol WITH carvedilol
Talk to your doctor before using carvedilol if you are also receiving treatment with albuterol. Carvedilol can sometimes cause severe narrowing of the airways and worsen your breathing problems. Carvedilol is normally not recommended if you have asthma, a history of asthma, or severe chronic obstructive pulmonary disease (COPD). Let your doctor know if you experience wheezing, shortness of breath, chest tightness, or other breathing difficulties if you do use these medications together. Your doctor or pharmacist may be able to suggest alternatives that do not interact. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.

Methyldopa WITH carvedilol
Ask your doctor before using carvedilol together with methyldopa. This can cause lead to a serious increase in your blood pressure. Call your doctor if you experience nausea, vomiting, sweating, flushing, stiff neck, headache, or heart palpitations. If you take both medications together, tell your doctor if you have any of these symptoms. You may need a dose adjustment or need your blood pressure checked more often if you take both medications. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.

Aminophylline WITH carvedilol
Ask your doctor before using carvedilol together with aminophylline. Using these medications together can make carvedilol less effective and increase the effects of aminophylline. Contact your doctor if you experience nausea, vomiting, insomnia, tremors, restlessness, uneven heartbeats, or difficulty breathing. If your doctor does prescribe these medications together, you may need a dose adjustment or special test to safely use both medications. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.

GENERALLY AVOID: The pharmacologic effects of theophyllines and beta-blockers are opposite. Nonselective and high doses of cardioselective beta-blockers may cause severe or fatal bronchospasm by opposing theophylline-induced bronchodilation. Ophthalmic beta-blockers undergo significant systemic absorption and may also interact. In addition, propranolol and other beta-blockers may reduce the CYP450 hepatic metabolism of theophylline, and serum theophylline levels may be increased.
MANAGEMENT: Oral and ophthalmic nonselective beta-blockers (e.g., carteolol, carvedilol, levobunolol, metipranolol, nadolol, oxprenolol, penbutolol, pindolol, propranolol, sotalol, and timolol) are considered contraindicated in patients with bronchospastic diseases. Cardioselective beta-blockers should generally be avoided, or used with extreme caution if no other alternatives are available and the benefits outweigh the risks of potentially severe bronchospasm. If patients do receive this combination, they should be closely monitored for increased serum theophylline levels but decreased bronchodilatory effectiveness.


Terbutaline WITH carvedilol
Talk to your doctor before using carvedilol if you are also receiving treatment with terbutaline. Carvedilol can sometimes cause severe narrowing of the airways and worsen your breathing problems. Carvedilol is normally not recommended if you have asthma, a history of asthma, or severe chronic obstructive pulmonary disease (COPD). Let your doctor know if you experience wheezing, shortness of breath, chest tightness, or other breathing difficulties if you do use these medications together. Your doctor or pharmacist may be able to suggest alternatives that do not interact. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.

GENERALLY AVOID: Beta-blockers may antagonize the effects of beta-2 adrenergic bronchodilators and precipitate acute, life-threatening bronchospasm in patients asthma or other obstructive airway diseases. The mechanism involves increased airway resistance and reduced bronchodilation due to blockade of beta-2 adrenergic receptors. The interaction may also occur with ophthalmically applied beta-blockers, which are systemically absorbed and can produce clinically significant systemic effects even at low or undetectable plasma levels. Due to opposing effects on beta-2 adrenergic receptors, propranolol has been used in the treatment of salbutamol overdose.

MANAGEMENT: The use of beta-2 adrenergic bronchodilators in combination with beta-blockers, including ophthalmic formulations, should generally be avoided. If concomitant use is required, a cardioselective beta-blocker (e.g., acebutolol, atenolol, betaxolol, bisoprolol, metoprolol, nebivolol) is usually preferred. Nevertheless, caution is advised and respiratory status should be closely monitored, as cardioselectivity is not absolute and larger doses of beta-1 selective agents may pose some of the same risks as nonselective agents. In general, nonselective beta-blockers are considered contraindicated in patients with obstructive airways disease.

CAPTOPRIL


Captopril  is an angiotensin-converting enzyme (ACE) inhibitor used for the treatment of hypertension and some types of congestive heart failure. Captopril was the first ACE inhibitor developed and was considered a breakthrough both because of its novel mechanism of action and also because of the revolutionary development process. Captopril is commonly marketed by Bristol-Myers Squibb under the trade name Capoten.
Captopril is a white to off-white crystalline powder that may have a slight sulfurous odor; it is soluble in water (approx. 160 mg/mL), methanol, and ethanol and sparingly soluble in chloroform and ethyl acetate.

CAPOTEN is available in potencies of 12.5 mg, 25 mg, 50 mg, and 100 mg as scored tablets for oral administration.



(2S)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]
pyrrolidine-2-carboxylic acid


USE AND DOSE

Captopril's main uses are based on its vasodilation and inhibition of some renal function activities. These benefits are most clearly seen in the following conditions:
1) Hypertension
2) Cardiac conditions such as congestive heart failure and after myocardial infarction
3) Preservation of kidney function in diabetic nephropathy
Additionally, it has shown mood-elevating properties in some patients. This is consistent with the observation that animal screening models indicate putative antidepressant activity for this compound, although there has been one negative study. Formal clinical trials in depressed patients have not been reported.
It has also been investigated for use in the treatment of cancer.
 BRANDS IN INDIA - ACETEN 25, ACETEN 12.5

Hypertension  -  Oral
Adult: Initially, 12.5 mg bid or 6.25 mg bid in combination with a diuretic, at bedtime to avoid precipitous fall in BP, gradually increased at 2-4-wk intervals according to response. Maintenance: 25-50 mg bid. Max: 50 mg tid.
Child: Neonate: Test dose: 10-50 mcg/kg (for neonates <37 1-12="" 1-2="" 10-50="" 100-300="" 100="" 10="" 12-18="" 12.5-25="" 150="" 1="" 2-3="" 2="" 300="" 4="" 6.25="" 6="" age:="" bp="" daily="" divided="" dose:="" doses.="" doses="" for="" give="" hr="" if="" in="" increased="" kg="" max:="" mcg="" mg="" monitor="" mth-12="" mth:="" nbsp="" needed.="" neonates="" or="" p="" postmenstrual="" test="" times="" tolerated="" wk="" yr:="">

Heart failure    -   Oral
Adult: Initially, 6.25-12.5 mg bid-tid. Maintenance: 25 mg bid-tid. Max: 50 mg tid.
Child: Neonate: Test dose: 10-50 mcg/kg (for neonates <37 1-12="" 1-2="" 10-50="" 100-300="" 100="" 10="" 12-18="" 12.5-25="" 150="" 1="" 2-3="" 2="" 300="" 4="" 6.25="" 6="" age:="" bp="" daily="" divided="" dose:="" doses.="" doses="" for="" give="" hr="" if="" in="" increased="" kg="" max:="" mcg="" mg="" monitor="" mth-12="" mth:="" needed.="" neonates="" or="" p="" postmenstrual="" test="" times="" tolerated="" wk="" yr:="">

Post myocardial infarction   -  Oral
Adult: May be started 3 days after MI. Initially, 6.25 mg/day increased after several wk to 150 mg daily in divided doses if tolerated.


Diabetic nephropathy   -   Oral
Adult: Proteinuria >500 mg per 24 hr (in patients with Type 1 diabetes mellitus and retinopathy): 25 mg tid. May be taken with other anti-hypertensives if patient requires further lowering of BP.
Child: Neonate: Test dose: 10-50 mcg/kg (for neonates <37 1-12="" 1-2="" 10-50="" 100-300="" 100="" 10="" 12-18="" 12.5-25="" 150="" 1="" 2-3="" 2="" 300="" 4="" 6.25="" 6="" age:="" bp="" daily="" divided="" dose:="" doses.="" doses="" for="" give="" hr="" if="" in="" increased="" kg="" max:="" mcg="" mg="" monitor="" mth-12="" mth:="" needed.="" neonates="" or="" p="" postmenstrual="" test="" times="" tolerated="" wk="" yr:="">
OVERDOSE   -  In case of overdose, call your local poison control center at 1-800-222-1222. If the victim has collapsed or is not breathing, call local emergency services at 911.

PREGNANCY - Do not take captopril if you are pregnant or breast-feeding. If you become pregnant while taking captopril, call your doctor immediately.


Special Populations: Patients with severe renal impairment: CrCl <30 12.5="" bid.="" initially="" mg="" min:="" ml="" p="">
Before taking captopril,
tell your doctor and pharmacist if you are allergic to captopril or any other drugs.
tell your doctor if you have diabetes (high blood sugar) and you are taking aliskiren (Tekturna, in Amturnide, Tekamlo, Tekturna HCT). Your doctor will probably tell you not to take captopril if you have diabetes and you are also taking aliskiren.
tell your doctor and pharmacist what prescription and nonprescription medications you are taking, especially diuretics ('water pills'), lithium (Eskalith, Lithobid), other medications for high blood pressure, potassium supplements, and vitamins.
tell your doctor if you have or have ever had heart or kidney disease or diabetes.
if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking captopril.


DRUG INTERACTIONS

captopril WITH  spironolactone
Using captopril together with spironolactone may increase the levels of potassium in your blood (hyperkalemia), especially if you are dehydrated or have kidney disease, diabetes, heart failure, or if you are an older adult. Hyperkalemia can cause symptoms such as weakness, confusion, numbness or tingling, and uneven heartbeats. If your doctor prescribes these medications together, you may need a dose adjustment or special tests to safely take both medications. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.

captopril WITH aliskiren
Using aliskiren together with captopril may increase potassium levels in the blood. High levels of potassium can develop into a condition known as hyperkalemia, which in severe cases can lead to kidney failure, muscle paralysis, irregular heart rhythm, and cardiac arrest. You may be more likely to develop hyperkalemia while using these medications if you are elderly, dehydrated, or have kidney disease, diabetes, or advanced heart failure. Regular or long-term use of nonsteroidal anti-inflammatory drugs such as ibuprofen or naproxen (Aleve) may also increase your risk. It is important that you maintain adequate fluid intake during treatment with these medications. Let your doctor know if you are diabetic or have kidney disease, as you may not be able to use these medications together. You should seek medical attention if you experience nausea, vomiting, weakness, confusion, tingling of the hands and feet, feelings of heaviness in the legs, a weak pulse, or a slow or irregular heartbeat, as these may be symptoms of hyperkalemia. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.


captopril WITH allopurinol
Talk to your doctor before using allopurinol together with captopril. Combining these medications may increase the risk of severe allergic reactions and infections. You should seek immediate medical attention if you develop shortness of breath; throat tightness; swelling of the face, lips, or tongue; itching; rash; fever; and/or muscle pain or weakness. Also let your doctor know if you notice signs of infection or experience fever, chills, sore throat, fatigue, body aches, or other flu-like symptoms. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.


captopril WITH amiloride
Using captopril together with aMILoride may increase the levels of potassium in your blood (hyperkalemia), especially if you are dehydrated or have kidney disease, diabetes, heart failure, or if you are an older adult. Hyperkalemia can cause symptoms such as weakness, confusion, numbness or tingling, and uneven heartbeats. If your doctor prescribes these medications together, you may need a dose adjustment or special tests to safely take both medications. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.



Wednesday, April 10, 2013

Candesartan


Candesartan  is an angiotensin II receptor antagonist used mainly for the treatment of hypertension. The prodrug candesartan cilexetil is marketed by AstraZeneca and Takeda Pharmaceuticals, commonly under the trade names Blopress, Atacand, Amias, and Ratacand.

2-ethoxy-1-({4-[2-(2H-1,2,3,4-tetrazol-5-yl)phenyl]phenyl}methyl)-1H-1,3-benzodiazole-7-carboxylic acid


USE
As all angiotensin II receptor antagonists, candesartan is indicated for the treatment of hypertension. Results from the CHARM study in the early 2000s demonstrated the morbidity and mortality reduction benefits of candesartan therapy in congestive heart failure. Thus, while ACE inhibitors are still considered first-line therapy in heart failure, candesartan can be used in combination with an ACE to achieve improved mortality and morbidity vs. an ACE alone and additionally is an alternative in patients intolerant of ACE inhibitor therapy.


DOSE :
Hypertension
Adult: Initially, 8 mg once daily adjusted according to response. Maintenance: 8 mg once daily. Max: 32 mg daily.
Renal impairment: For patients with renal impairment or on haemodialysis: Initially, 4 mg once daily.
Hepatic impairment: Initially, 2 mg once daily. Avoid in severe impairment.

Heart failure
Adult: Initially, 4 mg once daily, may double dose at intervals of not <2 32="" daily.="" max:="" mg="" nbsp="" p="" wk.="">Renal impairment: Reduce dose or discontinue treatment if renal function deteriorates.
Hepatic impairment: Initially, 2 mg once daily. Avoid in severe impairment.

Special Populations: Patients with renal and hepatic impairment: Initially, 2 mg once daily.

Special Precautions:  Volume or sodium depletion, preexisting renal insufficiency; aortic or mitral valve stenosis, hypertrophic obstructive cardiomyopathy, renal artery stenosis, primary hyperaldosteronism. Patients with a history of angioedema, urticaria. Monitor serum potassium levels especially in elderly and renally impaired patients. Hypotension may occur during major surgery and anaesthesia due to suppression of the renin-angiotensin system.

Sunday, April 7, 2013

Heartburn Trigger: Chocolate



Chocolate contains stimulants similar to caffeine, and caffeine can be a heartburn trigger. But if you can't bear the thought of giving up chocolate, see if cutting back helps you avoid heartburn. Watch your portion size, too; maybe you can handle a nibble. And keep the big picture in mind -- is that chocolate coming at the end of a fatty feast? Are you eating it by itself on an empty stomach? In short, what other heartburn triggers may be at play?


Heartburn Tip: Try Other Drinks



To make heartburn less likely, choose drinks that aren't fizzy and don't contain caffeine. Options include herbal teas, milk, and plain water. Having water with meals would also dilute stomach acid, making heartburn less likely. You may also want to limit tomato or citrus juices because of their acidity. And if you must have your coffee or other drinks that could promote heartburn, try to cut back -- maybe a smaller mug would help.


Drinks That May Trigger Heartburn



Preventing heartburn isn't just about food choices. Certain drinks can make heartburn more likely. Those beverages include coffee (regular or decaffeinated), caffeinated tea, colas, other carbonated drinks, and excess alcoholic beverages. Caffeinated beverages boost acid in the stomach and alcoholic beverages can relax the lower esophageal sphincter, leading to heartburn. And sodas, regardless of caffeine, can bloat the stomach, which may lead to heartburn.


Friday, April 5, 2013

Heartburn Tip: Limit Acidic Foods



You've got lots of other options for fresh produce besides tomatoes and citrus fruits. Try choosing some other fruits and vegetables. If you do want to have acidic foods, limit the portion size and have something else -- that isn't acidic -- with it. For instance, have a little less tomato sauce and have it with spaghetti and a little meat or vegetables at the same time. Everyone is different, so experiment to find your comfort zone.

Heartburn Trigger: Acidic Foods



Acidic foods -- which include tomatoes and products that contain tomatoes (such as tomato sauce and salsa) and citrus fruits (such as oranges, grapefruits, and lemons) -- can trigger heartburn, especially if you eat them by themselves, on an empty stomach. Vinegar is also highly acidic -- not that you're going to eat vinegar by itself, but it's a common ingredient in salad dressings and other dishes.

Monday, April 1, 2013

Heartburn Tip: Cut Back on Fat



You may not have to give up your favorite foods. Preparing them differently could help tame your heartburn. You might be able to bake, broil, grill, or roast some foods instead of frying them. And you could trim extra fat off meat and poultry, and cut the skin off chicken. Little tweaks might trim enough fat to make a difference for heartburn -- and your overall health.