Sunday, August 25, 2013

PROPRANOLOL

Propranolol is a beta-blocker. Beta-blockers affect the heart and circulation (blood flow through arteries and veins).

Propranolol is used to treat tremors, angina (chest pain), hypertension (high blood pressure), heart rhythm disorders, and other heart or circulatory conditions. It is also used to treat or prevent heart attack, and to reduce the severity and frequency of migraine headaches.


(RS)-1-(1-methylethylamino)-3-(1-naphthyloxy)propan-2-ol

USES
For,
Hypertension
Angina pectoris
Tachyarrhythmias
Myocardial infarction
Control of tachycardia/tremor associated with anxiety, hyperthyroidism or lithium therapy.
Essential tremor
Migraine prophylaxis
Cluster headaches prophylaxis
Tension headache (Off label use)
Shaky hands
Hyperhidrosis
There has been some experimentation in psychiatric areas:
Treating the excessive drinking of fluids in psychogenic polydipsia,
Antipsychotic-induced akathisia,
Aggressive behavior of patients with brain injuries
Post-traumatic stress disorder
Calming down individuals with phobias via sedative effects
Performance anxiety
Glaucoma
Thyrotoxicosis via deiodinase inhibition
Primary exertional headache
While once first-line treatment for hypertension, the role for beta-blockers was downgraded in June 2006 in the United Kingdom to fourth-line as they perform less well than other drugs, particularly in the elderly, and evidence is increasing that the most frequently used beta-blockers at usual doses carry an unacceptable risk of provoking type 2 diabetes.
Propranolol is also used to lower portal vein pressure in portal hypertension and prevent esophageal variceal bleeding and ascites.


MECHANISM OF ACTION
Propranolol is a non-selective beta blocker, that is, it blocks the action of epinephrine and norepinephrine on both β1- and β2-adrenergic receptors. It has little intrinsic sympathomimetic activity (ISA) but has strong membrane stabilizing activity (only at high blood concentrations, e.g. overdosage). Research has also shown that propranolol has inhibitory effects on the norepinephrine transporter and/or stimulates norepinephrine release (present experiments have shown that the concentration of norepinephrine is increased in the synapse but do not have the ability to discern which effect is taking place).[31] Since propranolol blocks β-adrenoceptors, the increase in synaptic norepinephrine only results in α-adrenergic activation, with the α1-adrenoceptor being particularly important for effects observed in animal models. Therefore, some have suggested that it be looked upon as an indirect α1 agonist as well as a β antagonist. Probably owing to the effect at the α1-adrenoceptor, the racemic and the individual enantiomers of propranolol have been shown to substitute for cocaine in rats, with the most potent enantiomer being S-(–)-propranolol. In addition, some evidence suggests that propranolol may function as a partial agonist at one or more serotonin receptors (possibly 5-HT1B).
Both enantiomers of the drug have a local anesthetic (topical) effect, which is normally mediated by blockade of voltage-gated sodium channels. Few studies have demonstrated propranolol's ability to block cardiac, neuronal, and skeletal voltage-gated sodium channels, accounting for its known "membrane stabilizing effect" and anti-arrhythmic and other central nervous system effects.

Important information about propranolol :

You should not use this medication if you are allergic to propranolol, if you have asthma, a slow heart rate, or a serious heart condition such as "sick sinus syndrome" or "AV block" (unless you have a pacemaker). If you need surgery, tell the surgeon ahead of time that you are using propranolol. You may need to stop using the medicine for a short time. Do not skip doses or stop using propranolol without first talking to your doctor. You may need to use less and less before you stop the medication completely.
Avoid drinking alcohol. It may increase your blood levels of propranolol.

Propranolol is only part of a complete program of treatment for hypertension that may also include diet, exercise, and weight control. Follow your diet, medication, and exercise routines very closely if you are being treated for hypertension.

If you are being treated for high blood pressure, keep using propranolol even if you feel well. High blood pressure often has no symptoms. You may need to use blood pressure medication for the rest of your life.


DOSAGES

Usual Adult Propranolol Dose for Hypertension:

Initial dose: 40 mg orally twice a day or 80 mg sustained release once a day, whether used alone or added to a diuretic. The dose should be administered at bedtime (approximately 10 PM).
Maintenance dose: 120 to 240 mg/day or 120 to 160 mg/day of sustained release
Maximum dose: 640 mg/day.

Usual Adult Propranolol Dose for Angina Pectoris:

Total daily doses of 80 to 320 mg orally 2 to 4 times a day have been shown to increase exercise tolerance and to reduce ischemic changes in the ECG.
Sustained release: Initial dose: 80 mg orally once a day. Dosage should be gradually increased at 3 to 7 day intervals. The average optimal dosage appears to be 160 mg/day.

Usual Adult Propranolol Dose for Arrhythmias:

Oral: 10 to 30 mg 3 to 4 times a day, before meals and at bedtime.
IV: 1 to 3 mg at a rate not exceeding 1 mg/min.
Sufficient time should be allowed for the drug to reach the site of action even when a slow circulation is present. A second dose may be given after 2 minutes. Thereafter, additional drug should not be given in less than 4 hours. Additional propranolol should not be given when the desired alteration in rate and/or rhythm is achieved.

Usual Adult Propranolol Dose for Myocardial Infarction:

180 to 240 mg/day in 3 to 4 divided doses.

Usual Adult Propranolol Dose for Migraine Prophylaxis:

Initial dose: 80 mg/day orally in divided doses.
Maintenance dose: 160 to 240 mg/day.
The dosage may be increased gradually to achieve optimum migraine prophylaxis. If a satisfactory response is not obtained within 4 to 6 weeks after reaching the maximum dose, propranolol therapy should be discontinued.
Sustained release: Initial dose: 80 mg orally once a day.
Maintenance dose: 160 to 240 mg once a day.

Usual Adult Propranolol Dose for Benign Essential Tremor:

Initial dose: 40 mg orally twice a day.
Maintenance dose: 120 to 320 mg/day.
Optimum reduction of essential tremor is usually achieved with a dose of 120 mg/day.
Occasionally, it may be necessary to administer 240 to 320 mg/day.

Usual Adult Propranolol Dose for Aortic Stenosis:

20 to 40 mg orally 3 to 4 times a day, before meals and at bedtime.
Sustained release: 80 to 160 mg orally once a day.

Usual Adult Propranolol Dose for Pheochromocytoma:

Preoperatively: 60 mg/day orally in divided doses for 3 days prior to surgery, concomitantly with an alpha-adrenergic blocking agent.
Management of Inoperable Tumor: 30 mg/day orally in divided doses.

Usual Pediatric Propranolol Dose for Arrhythmias:

Oral: Children: Initial: 0.5 to 1 mg/kg/day in divided doses every 6 to 8 hours; titrate dosage upward every 3 to 5 days; usual dose: 2 to 4 mg/kg/day; higher doses may be needed; do not exceed 16 mg/kg/day

IV: Children: 0.01 to 0.1 mg/kg slow IV over 10 minutes; maximum dose: 1 mg (infants); 3 mg (children).

Usual Pediatric Propranolol Dose for Hypertension:

Children:
Immediate release formulations:
Initial: 0.5 to 1 mg/kg/day in divided doses every 6 to 12 hours; increase gradually every 5 to 7 days
Usual dose: 1 to 5 mg/kg/day
Maximum dose: 8 mg/kg/day

Children and Adolescents 1 to 17 years:
Immediate release formulations:
Initial: 1 to 2 mg/kg/day divided in 2 to 3 doses/day; titrate dose to effect
Maximum dose: 4 mg/kg/day up to 640 mg/day; sustained release formulation may be dosed once daily. (National High Blood Pressure Education Program Working Group on High Blood Pressure in Children and Adolescents).

Usual Pediatric Propranolol Dose for Thyrotoxicosis:

Neonates: Oral: 2 mg/kg/day in divided doses every 6 to 12 hours; occasionally higher doses may be required.

Adolescents: Oral: 10 to 40 mg/dose every 6 hours.


BRANDS

Beptazine           Propranolol, Dihydralazine Sulphate                           M.M.LABS
Beptazine -H        Propranolol, Dihydralazine Sulphate,Hydrochlorothiazide       M.M LABS
Betaprp -DZ         Propranolol, Diazepam                                         Consern Pharma Pvt Ltd.
ciplar 10                proranolol                                                    cipla
inderal 10
Avlocardyl, Deralin, Dociton, Inderalici, InnoPran XL, Sumial, Anaprilinum, Bedranol SR



Thursday, August 22, 2013

PRAZOSIN

Prazosin  is a sympatholytic drug used to treat high blood pressure and anxiety, PTSD, and panic disorder. It is an alpha-adrenergic blocker that is specific for the alpha-1 receptors. These receptors are found on vascular smooth muscle, where they are responsible for the vasoconstrictive action of norepinephrine. They are also found throughout the central nervous system.
In addition to its alpha-blocking activity, prazosin is an antagonist of the MT3 receptor (which is not present in humans), with selectivity for this receptor over the MT1 and MT2 receptors.

Prazosin is orally active and has a minimal effect on cardiac function due to its alpha-1 receptor selectivity. However, when prazosin is initially started, heart rate and contractility go up in order to maintain the pre-treatment blood pressures because the body has reached homeostasis at its abnormally high blood pressure. The blood pressure lowering effect becomes apparent when prazosin is taken for longer periods of time. The heart rate and contractility go back down over time and blood pressure decreases.
The antihypertensive characteristics of prazosin make it a second-line choice for the treatment of high blood pressure.
Prazosin is also useful in treating urinary hesitancy associated with prostatic hyperplasia, blocking alpha-1 receptors, which control constriction of both the prostate and ureters. Although not a first line choice for either hypertension or prostatic hyperplasia, it is a choice for patients who present with both problems concomitantly
This medication has shown to be effective in treating severe nightmares in children and people with PTSD symptoms.[4] Veterans have also been treated successfully at Seattle's VA Puget Sound Health Care System (VAPSHCS) for sleep disturbance related to PTSD. Doses are lower for this purpose than for control of blood pressure.

2-[4-(2-furoyl)piperazin-1-yl]-6,7-dimethoxyquinazolin-4-amine

BRAND NAMES  -
Mizide
Cyber-cr           Raptakos
Czopress XL Tab    CMG Biotech
Minipress Xl       Pfiser
Minipress Xl ITS   Pfiser
Prazocip -1 tab    Cipla
 Prazocip XL       Cipla
Prazopress         Sun pharma
Prazopress XL      Sun
Prazopress 1       sun
Prazopress 2       sun
Prazopress XL 5    Sun


Do NOT use prazosin if:
you are allergic to any ingredient in prazosin
Contact your doctor or health care provider right away if any of these apply to you.

Before using prazosin:

Some medical conditions may interact with prazosin. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:

if you are pregnant, planning to become pregnant, or are breast-feeding
if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement
if you have allergies to medicines, foods, or other substances
if you have chest pain, heart disease, narcolepsy, or kidney problems
if you will be having eye surgery
Some MEDICINES MAY INTERACT with prazosin. Tell your health care provider if you are taking any other medicines, especially any of the following:

Diuretics (eg, furosemide, hydrochlorothiazide) or verapamil because they may increase the risk of prazosin's side effects
Beta-blockers (eg, propranolol) or phosphodiesterase inhibitors (eg, sildenafil) because their actions and the risk of their side effects may be increased by prazosin
This may not be a complete list of all interactions that may occur. Ask your health care provider if prazosin may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.

How to use prazosin:

Use prazosin as directed by your doctor. Check the label on the medicine for exact dosing instructions.

Take prazosin by mouth with or without food.
If you miss a dose of prazosin, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once.
Ask your health care provider any questions you may have about how to use prazosin.

Important safety information:

Prazosin may cause dizziness, lightheadedness, or fainting after the first dose. Take the first dose at bedtime. If you get up during the night, sit up and stand slowly. Continue to sit up and stand slowly while you are taking prazosin.
Prazosin may cause dizziness, drowsiness, lightheadedness, or blurred vision. These effects may be worse if you take it with alcohol or certain medicines. Use prazosin with caution. Do not drive or perform other possibly unsafe tasks until you know how you react to it.
Prazosin may cause dizziness, lightheadedness, or fainting; alcohol, hot weather, exercise, or fever may increase these effects. To prevent them, sit up or stand slowly, especially in the morning. Sit or lie down at the first sign of any of these effects.
Avoid engaging in any hazardous tasks for at least 24 hours after taking the first dose, missing several doses, increasing the dose, or taking other high blood pressure medications.
Before drinking alcohol, discuss it with your doctor.
Tell your doctor or dentist that you take prazosin before you receive any medical or dental care, emergency care, or surgery.
Patients who take medicine for high blood pressure often feel tired or run down for a few weeks after starting treatment. Be sure to take your medicine even if you may not feel "normal." Tell your doctor if you develop any new symptoms.
Prazosin may interfere with certain lab tests, including tests for pheochromocytoma (an adrenal gland tumor). Be sure your doctor and lab personnel know you are taking prazosin.
Use prazosin with extreme caution in the ELDERLY; they may be more sensitive to its effects.
Prazosin should not be used in CHILDREN; safety and effectiveness in children have not been confirmed.
PREGNANCY and BREAST-FEEDING: If you become pregnant, contact your doctor. You will need to discuss the benefits and risks of using prazosin while you are pregnant. Prazosin is found in breast milk. If you are or will be breast-feeding while you use prazosin, check with your doctor. Discuss any possible risks to your baby.

Possible side effects of prazosin:
All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome:

Dizziness; drowsiness; dry mouth; frequent urination; headache; lack of energy; lightheadedness; nasal congestion; nausea; weakness.

Seek medical attention right away if any of these SEVERE side effects occur:
Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); blurred vision; fainting; fast or irregular heartbeat; depression; severe or persistent dizziness; swelling of the hands or feet.

This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.


Sunday, August 18, 2013

PHENOXYBENZAMINE

This medication is used to treat high blood pressure and heavy sweating due to a certain tumor of the adrenal glands (pheochromocytoma). Phenoxybenzamine belongs to a class of drugs known as alpha blockers. It works by relaxing and widening blood vessels so that blood can flow more easily.
OTHER USES: This section contains uses of this drug that are not listed in the approved professional labeling for the drug but that may be prescribed by your health care professional. Use this drug for a condition that is listed in this section only if it has been so prescribed by your health care professional.
This drug may also be used with other medications to treat certain blood circulation problems (e.g., Raynaud's syndrome).
It is also used to treat certain conditions which involve difficulty urinating (e.g., neurogenic bladder, partial prostatic obstruction).

alpha adrenergic blocker   .


(RS)-N-benzyl-N-(2-chloroethyl)-1-phenoxypropan-2-amine

PHARMACOLOGY
Phenoxybenzamine is used as an anti-hypertensive due to its efficacy in reducing the vasoconstriction caused by epinephrine (adrenaline) and norepinephrine. Phenoxybenzamine forms a permanent covalent bond with adrenergic receptors. Based on known information about the structures of these receptors, it likely involves attack by the cysteine at position 3.36 in transmembrane helix 3 to form a stable linkage. Thus, it remains permanently bound to the receptor, preventing adrenaline and noradrenaline from binding. This causes vasodilatation in blood vessels, due to its antagonistic effect at the alpha-1 adrenoceptor found in the walls of blood vessels, resulting in a drop in blood pressure. A side effect of phenoxybenzamine is reflex tachycardia.
It will also affect the postsynaptic alpha 1 and 2 receptors in the nervous system, and so reduce sympathetic activity. This results in further vasodilation, pupil constriction, an increase in GI tract motility and secretions, and glycogen synthesis.
It also has partial agonist/antagonist properties at the serotonin 5-HT2A receptor. Due to its 5-HT2A antagonism, it is useful in the treatment of carcinoid tumor, a neoplasm that secretes large amounts of serotonin and causes diarrhea, bronchoconstriction, and flushing.


DOSE

The dose of phenoxybenzamine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of phenoxybenzamine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

For oral dosage form (capsules):
For high blood pressure caused by pheochromocytoma:
Adults—At first, 10 milligrams (mg) two times a day. Then, your doctor may increase your dose to 20 to 40 mg two or three times a day.
Children—Dose is based on body weight and must be determined by your doctor. The usual starting dose is 0.2 mg per kilogram (kg) (0.09 mg per pound) of body weight taken once a day. Then, your doctor may increase your dose to 0.4 to 1.2 mg per kg (0.18 to 0.55 mg per pound) of body weight a day. This is divided into three or four doses.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.
Keep out of the reach of children.
Do not keep outdated medicine or medicine no longer needed.


SPECIAL PRECAUTIONS
tell your doctor and pharmacist if you are allergic to phenoxybenzamine or any other drugs.
tell your doctor and pharmacist what prescription and nonprescription medications you are taking, especially medications for diet control, high blood pressure, asthma, cough, colds, allergies, and glaucoma; and vitamins.
tell your doctor if you have or have ever had heart or kidney disease, a stroke, or transient ischemic attacks (TIA).
tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant while taking phenoxybenzamine, call your doctor immediately.
if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking phenoxybenzamine.
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.



SIDE EFFECTS

Phenoxybenzamine may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:
nasal congestion  , dizziness  , upset stomach  , sexual dysfunction (difficulty ejaculating)  , dizziness

If you experience any of the following symptoms, call your doctor immediately:
fainting  , fast heartbeat    , vomiting

If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration's (FDA) MedWatch Adverse Event Reporting program online [at http://www.fda.gov/Safety/MedWatch] or by phone [1-800-332-1088].




DRUG INTERACTIONS
Using phenoxybenzamine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

Acebutolol
Alprenolol
Atenolol
Betaxolol
Bevantolol
Bisoprolol
Bucindolol
Carteolol
Carvedilol
Celiprolol
Dilevalol
Esmolol
Labetalol
Levobunolol
Mepindolol
Metipranolol
Metoprolol
Nadolol
Nebivolol
Oxprenolol
Penbutolol
Pindolol
Propranolol
Sotalol
Talinolol
Tertatolol
Timolol
Vardenafil

BRANDS

Dibenzyline

China - 2 Results
酚苄明/phenoxybenzamine
酚苄明 - 丽珠制药/Phenoxybenzamine - Livzon  [ 丽珠制药厂 / Livzon Pharm ]
India - 4 Results
BIOPHENOX  [ United Biotech ]
FENOBEN  [ Celon (Revilon) ]
FENOXENE  [ Samarth ]
phenoxybenzamine
Indonesia - 1 Results
phenoxybenzamine
Hong Kong - 1 Results
phenoxybenzamine
Malaysia - 1 Results
phenoxybenzamine
Philippines - 1 Results
phenoxybenzamine
Singapore - 1 Results
phenoxybenzamine
Thailand - 2 Results
Adrenaline Atlantic  [ Atlantic Lab ]   [ Vana ]
phenoxybenzamine
Vietnam - 0 Results
USA - 2 Results
Demser  [ Merck & Co Inc ]
phenoxybenzamine



Sunday, August 11, 2013

PERINDOPRIL


Perindopril is comes under the group of long-acting ACE inhibitor. It is used to treat high BP, heart failure or stable coronary artery disease in form of perindopril arginine  or perindopril erbumine. According to the Australian government's Pharmaceutical Benefits Scheme website, based on data provided to the Australian Department of Health and Aging by the manufacturer, perindopril arginine and perindopril erbumine are therapeutically equivalent and may be interchanged without differences in clinical effect. However the dose prescribed to achieve the same effect will differ due to different molecular weights for the two forms.
Perindopril is used alone or in combination with other medications to treat high blood pressure. Perindopril is in a class of medications called angiotensin-converting enzyme (ACE) inhibitors. It makes blood flow more smoothly by preventing the production of certain natural chemicals that tighten the blood vessels.
Perindopril comes as a tablet to take by mouth. It is usually taken once or twice a day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take perindopril exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.
Your doctor may start you on a low dose of perindopril and gradually increase your dose.
Perindopril controls high blood pressure but does not cure it. Continue to take perindopril even if you feel well. Do not stop taking perindopril without talking to your doctor.




SPECIAL PRECAUTIONS
Before taking perindopril,
Tell your doctor and pharmacist if you are allergic to perindopril, benazepril (Lotensin), captopril (Capoten), enalapril (Vasotec), fosinopril (Monopril), lisinopril (Prinivil, Zestril), moexipril (Univasc), quinapril (Accupril), ramipril (Altace), trandolapril (Mavik), or any other medications.
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 perindopril if you have diabetes and you are also taking aliskiren.
tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking. Be sure to mention any of the following: cyclosporine (Neoral, Sandimmune), diuretics ('water pills'), heparin, indomethacin (Indocin), lithium (Eskalith, Lithobid), and potassium supplements (K-Dur, Klor-Con, others). Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
tell your doctor if you are on dialysis and if have or have ever had heart failure; lupus (SLE); scleroderma; diabetes; swelling of the face, throat, tongue, lips, eyes, hands, feet, ankles, and/or lower legs (angioedema); or kidney or liver disease.
tell your doctor if you plan to become pregnant or are breast-feeding.
you should know that diarrhea, vomiting, not drinking enough fluids, and sweating a lot can cause a drop in blood pressure, which may cause lightheadedness and fainting.
DIET
Talk to your doctor before using salt substitutes containing potassium. If your doctor prescribes a low-salt or low-sodium diet, follow these directions carefully.
IF YOU FORGOT YOUR DOSE...
Take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.
SIDE EFFECTS
Perindopril may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:
Cough,  headache,  weakness,  dizziness,  diarrhea,  stomach pain,  upset stomach
Some side effects can be serious. The following symptoms are uncommon, but if you experience any of them, call your doctor immediately:
swelling of the face, throat, tongue, lips, eyes, hands, feet, ankles, or lower legs
hoarseness,  difficulty swallowing or breathing,  lightheadedness,  fainting
fever, sore throat, chills, and other signs of infection
irregular or rapid heartbeats
Perindopril may cause other side effects. Call your doctor if you have any unusual problems while taking this medication.


If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration's (FDA) MedWatch Adverse Event Reporting program online [at http://www.fda.gov/Safety/MedWatch] or by phone [1-800-332-1088].

Sunday, August 4, 2013

NITRENDIPINE

Nitrendipine is a dihydropyridine calcium channel blocker. It is used in the treatment of primary hypertension.


ethyl methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate


Nitrendipine is absorbed through gut and metabolized by liver before it goes into the systemic circulation and reaches the cells of the smooth muscles and cardiac muscle cells.
 It binds more effectively with L-type calcium channels in smooth muscle cells because of its lower resting membrane potential. The Nitrendipine diffuses into the membrane and binds to its high affinity binding site on the inactivated L-type calcium channel that’s located in between each of the 4 intermembrane components of the α1 subunit. The exact mechanism of action of Nitrendipine is unknown, but it is believed to have important tyrosine and threonine residues in its binding pocket and its binding interferes with the voltage sensor and gating mechanism of the channel. Thought to have a domain-interface model of binding. In hypertension, the binding of Nitrendipine causes a decrease in the probability of open L-type calcium channels and reduces the influx of calcium. The reduced levels of calcium prevent smooth muscle contraction within these muscle cells. Prevention of muscle contraction enables smooth muscle dilation. Dilation of the vasculature reduces total peripheral resistance, which decreases the workload on the heart and prevents scarring of the heart or heart failure.

INDICATION AND DOSE
Hypertension
Adult: 20 mg daily as a single dose or in 2 divided doses; may be increased to 20 mg bid as necessary to control resistant hypertension.
Elderly: Initially, 10 mg daily.
Hepatic impairment: Initially, 5-10 mg once daily.
OVERDOSAGE
Symptoms: Flushing, headache, BP reduction with circulatory collapse, changes in heart rate (tachycardia, bradycardia). Management: Initially, gastric lavage with subsequent activated charcoal. Dopamine or noradrenaline may be used for excessive hypotension. Atropine or orciprenaline may be used for bradycardia.
ADVERSE DRUG REACTIONS
Hypotension, flushing, oedema, dizziness, palpitation, fatigue, headache, nausea, bloating, diarrhoea, paraesthesias, tachycardia, asthenia, drowsiness, angina, MI, irritability, respiratory disorders, hypersensitivity reactions, increased urine output, elevated LFTs, myalgia, tremor, blood count changes, gingival hyperplasia.
DRUG INTERACTIONS
Effects may be enhanced by other antihypertensives. Increased sodium excretion with diuretics at the start of treatment. May prolong effects of pancuronium, vecuronium. May increase digoxin levels. Reduced levels/effects with rifampicin, phenytoin, carbamazepine or phenobarbitone. Levels/effects may be increased with cimetidine, valproic acid, erythromycin, troleandomycin, clarithromycin, roxithromycin, ketoconazole, itraconazole, fluconazole, nefazodone, protease inhibitors, quinupristin or dalfopristin.
Potentially Fatal: Effects may be enhanced by other antihypertensives. Increased sodium excretion with diuretics at the start of treatment. May prolong effects of pancuronium, vecuronium. May increase digoxin levels. Reduced levels/effects with rifampicin, phenytoin, carbamazepine or phenobarbitone. Levels/effects may be increased with cimetidine, valproic acid, erythromycin, troleandomycin, clarithromycin, roxithromycin, ketoconazole, itraconazole, fluconazole, nefazodone, protease inhibitors, quinupristin or dalfopristin.

FOOD INTERACTIONS  -    Concentration may be increased with grapefruit juice.

BRANDS                  -      COMPANY  -  COUNTRY
Balodipine                          Taiyo Pharmaceutical, Japan
Balotein                               Medisa Shinyaku, Japan
Baylotensin                        Tanabe Mitsubishi Pharma, Japan
Bayniroad                           Taisho Yakuhin, Japan
Bayotensin                         Bayer Vital, Germany
Bayotensin mite              Bayer Vital, Germany
Baypresol                            Bayer, Spain
Baypress                              Bayer, Austria;   Bayer, Belgium;   Bayer, Switzerland;    Bayer, Colombia;     Bayer, Czech Republic;       Bayer, Denmark;       Bayer, Greece;     Bayer, Hungary;      Bayer, Italy;      Bayer, South Korea;          Bayer, Netherlands;      Bayer, Thailand;       Bayer, Turkey;     Bayer Animal Health, Luxembourg;      Bayer Santé, France
Baypress mite                   Bayer, Switzerland
Caltren                                 Libbs, Brazil
Cardiazem                          Sanitas, Chile
Cenipres (Nitrendipine and Enalapril)- Ferrer, Austria
Cobatensin                         Kobayashi Kako, Japan
Ditrenil                                                Siam Bheasach, Thailand
Dosperopin                        Towa Yakuhin, Japan
Ecatelisin            Zensei Yakuhin, Japan
Ellenal                  Sanwa Kagaku, Japan
Eneas (Nitrendipine and Enalapril)  -  Abbott, Turkey; Dream Pharma, South Korea; Ferrer, Dominican Republic; Ferrer, Guatemala; Ferrer, Honduras; Ferrer, Luxembourg; Ferrer, Nicaragua; Ferrer, El Salvador; Ferrer Farma, Spain; Galenica, Greece; Galenica, Romania
ENEAS (Nitrendipine and Enalapril)- Ferrer, Germany; Merck, Germany
Enit (Nitrendipine and Enalapril) - Adeka, Turkey;   Ferrer, Luxembourg;    Ferrer Farma, Spain;     Gap, Greece
Gericin                                 Seid, Spain
Grifonitren                         Chile, Chile
Jutapress                             Juta, Germany; Q-Pharm, Germany
Leonitren                            Mentinova, Greece
Lisba                                      Rafarm, Greece
Lostradyl                             Chrispa, Greece
Lusopress                            Berlin-Chemie, Bulgaria;   Berlin-Chemie, Estonia;   Instituto Luso Farmaco, Czech Republic;     Luso, Latvia;     Lusofarmaco, Lithuania;      Lusofarmaco, Romania;      Lusofarmaco, Slovakia;       Lusofarmaco, Tunisia
Miniten                               Utopian, Thailand
Nelconil                               Pharmathen, Greece
Nian                                      Ying Yuan, Taiwan
Nidrel                                   UCB Pharma, France
Nifecard                              Bros, Greece
Nilzipin                                                Kyorin Rimedio, Japan
Niprina                                 Esteve, Spain
Nirapel                                 Ivax, Argentina
Nitopress                            Kyowa Yakuhin, Japan
Nitotelocin                         Choseido Pharmaceutical, Japan
Nitregamma                      Wörwag Pharma, Germany
Nitren Lich                          Winthrop, Germany
Nitren                                   Siu Guan, Taiwan
Nitren-acis                         Acis, Germany
Nitrencord                          Biosintética, Brazil
Nitrend KSK                       KSK-Pharma, Germany
Nitrendil                             Bagó, Argentina; Elmor, Venezuela
Nitrendilat                                         Medilat, Greece
Nitrendipin - 1 A Pharma             1A Pharma, Germany
Nitrendipin AbZ                               AbZ-Pharma, Germany
Nitrendipin Actavis                        Actavis, Germany; Balkanpharma, Bulgaria
Nitrendipin AL                                  Aliud, Bulgaria; Aliud, Germany
Nitrendipin Aristo                           Aristo Pharma, Germany
Nitrendipin Basics                           Basics, Germany
Nitrendipin beta                              Betapharm, Germany
Nitrendipin dura                              Mylan dura, Germany
Nitrendipin Heumann                          Heumann, Germany
Nitrendipin JENAPHARM                             mibe, Germany
Nitrendipin Lindopharm                              Lindopharm, Germany
Nitrendipin Sandoz                                      Sandoz, Germany
Nitrendipin STADA                STADA, Germany
Nitrendipin-corax                   Corax, Germany
Nitrendipin-CT                           CT Arzneimittel, Germany
Nitrendipine - Pacific Pharm - Pacific, China
Nitrendipine Myla                    Mylan, France
Nitrendipine Teva                 Teva Santé, France
Nitrendipine Xinhua Pharm - Xinhua, China
Nitrendipine-Xinhua Pharm -  Xinhua, China
Nitrendipino Andromaco   Andromaco, Chile
Nitrendipino L.CH.               Chile, Chile
Nitrendipino Mintlab          Mintlab, Chile
Nitrendipino Ratiopharm   Ratiopharm, Spain
Nitrendipino Rider           Rider, Chile
Nitrendipino Stada           STADA, Spain
Nitrendipin-ratiopharm  Ratiopharm, Germany; Ratiopharm, Czech Republic
Nitrendypina Anpharm   Anpharm, Poland
Nitrensal                             TAD, Germany
Nitrepin                               Zdravlje, Serbia
Nitrepress                          Hexal, Czech Republic; Hexal, Germany; Hexal, Lithuania
Nitre-Puren                       Actavis, Germany
Nitresan                              Pro.Med., Poland; Pro.Med.CS, Czech Republic; Pro.Med.CS, Estonia; Pro.Med.CS, Lithuania; Pro.Med.CS, Slovakia
Nitrezic                                                Ohara Yakuhin, Japan
Nivitron                               Coup, Greece
Potional                               Kleva, Greece
Ravena                                 STADA, Bulgaria
Shetlazorna                        Nisshin Seiyaku - Yamagata, Japan
Shu Mai Te                         Great Wall Pharmaceutical Factory, China
Spidox               Finixfarm, Greece
Tensogradal           Kern, Spain
Tepanil   -           Norma Hellas, Greece
Unipres   -              Krka, Czech Republic; Krka, Hungary; Krka, Lithuania; Krka, Slovenia
Unipress  -                  Krka, Slovakia
Vastensium    -           Salvat, Spain

Vipres (Nitrendipine and Enalapril)  -  Ferrer Farma, Spain