Sunday, April 20, 2014

RAMIPRIL

Ramipril is an angiotensin-converting enzyme (ACE) inhibitor, used to treat high blood pressure and congestive heart failure.

USE

Hypertension;
Congestive heart failure;
Following heart attack in patients with clinical evidence of heart failure;
Susceptible patients over 55 years: prevention of heart attack, stroke, cardiovascular death or need of revascularization procedures.
Diabetic nephropathy (kidney damage due to diabetes) with microalbuminuria (protein in the urine); in low doses it is used as a prophylaxis for developing nephropathy and related secondary cardiovascular events.

DOSING: The usual dose of ramipril for hypertension is 2.5-20 mg a day as a single dose or two divided doses. Patients taking diuretics or who have reduced kidney function may require lower doses. Heart failure is initially treated with 1.25-2.5 mg twice daily then titrated up to 10 mg once daily or 5 mg twice daily. The dose for preventing heart attacks and strokes is 2.5-10 mg daily.


IUPAC Name     -  (2S,3aS,6aS)-1-[(2S)-2-{[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino}propanoyl]-octahydrocyclopenta[b]pyrrole-2-carboxylic acid


STORAGE: Tablets and capsules should be stored at room temperature between 15 C to 30 C (59 F to 86 F).

CONTRA INDICATIONS  -  Renovascular disease (impaired blood flow in the kidneys), severe renal impairment (especially in patients with one kidney or with bilateral renal artery stenosis), volume-depleted patients, history of angioedema while on an ACE inhibitor, pregnancy, hypotension.


ADVERSE EFFECTS  -
low blood sugar (in patients taking medication for diabetes), causing sweating or shakiness
dry cough
dizziness and light-headedness due to low blood pressure
tiredness and fatigue, especially in the early stages
mouth dryness in the early stages
nausea, vomiting, diarrhea (persistent in rare cases)
fainting
change in amount of urine
signs of infection (e.g., fever, chills, persistent sore throat)
yellowing of eyes or skin, dark urine
stomach or abdominal pain
neutropenia (low white blood cells)
impotence (erectile dysfunction)
Serious allergic reactions to this drug are unlikely, but immediate medical attention must be sought if they occur. Symptoms of a serious allergic reaction include, but are not limited to a rash or swelling of the face, mouth, tongue, or throat.

In extreme cases, ramipril may lead to potentially fatal liver problems.


MECHANISM OF ACTION  -
ACE inhibitors, as the name suggests, inhibit the actions of angiotensin converting enzyme (ACE), thereby lowering the production of angiotensin II and also decreasing the breakdown of bradykinin. The decrease in angiotensin II results in relaxation of arteriole smooth muscle leading to a decrease in total peripheral resistance, reducing blood pressure as the blood is pumped through widened vessels. Its effect on bradykinin is responsible for the dry cough side effect.

Ramipril, a prodrug or precursor drug, is converted to the active metabolite (metabolic product) ramiprilat by liver esterase enzymes.[4] Ramiprilat is mostly excreted by the kidneys. The half-life of ramiprilat is variable (3–16 hours), and is prolonged by heart and liver failure, as well as kidney failure.

DRUG INTERACTIONS: The use of ACE inhibitors with potassium supplements, salt substitutes or diuretics (for example, spironolactone [Aldactone] that increase potassium in the blood may lead to excessive potassium levels. Potassium levels should be monitored whenever ACE inhibitors are used in combination with these drugs.


PATENT -
The compound was protected by U.S. Patent 5,061,722 which was assigned to Aventis on 29 October 1991. The patent was scheduled to expire on 29 October 2008. On 11 September 2007, in an appeal by the Indian company Lupin Ltd., the United States Court of Appeals for the Federal Circuit reversed a district court trial verdict and found that Aventis's patent on ramipril was invalid for "obviousness" - opening this medicine to generic manufacturers.

Ramipril is marketed in India under the brand names of Cardace, Zigpril, Ramistar and Zorem.

BRANDS
Artere Tabet                  Valiant Healthcare Limited
Artere (5 mg) Tabet         Alchemist Lifesciences Ltd.
Cardace Tabet              Alcare David Ltd.
Cardiopril Cap                Dr. Reddy s Laboratories
Conram Tabet              Concertina Pharma Pvt. Ltd
Cordimil Cap                Ind - Swift
Corpril Cap                     Ranbaxy
Dexace (10 mg) Tabet     Dexter Laboratories Pvt. Ltd.
Ecator (10 mg) Tabet       Torrent Labs (P) Ltd.
G -Pril Tabet               Hinglaj Labs of India
Gopril (10 mg)Tabet         CMG Biotech
GR Pace (10 mg)Tabet     G R Laboratories Pvt. Ltd.
Hopace Tab                 Micro Labs Ltd (Cardicare)
Hoperam(1.25mg)Tabet   Zinnia Life Sciences
Kepry Tabet                 Cadex Laboratories
Megapril Tabet                 Biomax
Misry Tabet                 Biocin Healthcare
Nexrami Tabet               Nexus Biotech
Panpril -5 Tabet               Panvik Pharmaceuticals
Polypril (10mg)Tabet       Druto Laboratories
Preface Tabet               Centaur Pharmaceuticals Pvt.Ltd.
Proace (2.5mg)Tabet       Alembic Chemical Works Co Ltd
Race (1.25mg)Tablet       Alkem Laboratories Ltd
Ramace (10mg)Cap         Astra Zeneca Pharma India Limited
Ramcor 5 Cap                 IPCA Laboratories (Innova Division)
Ramey Cap                Cadila Pharmaceuticals (Recon Healthcare)
Rami -Ten tab                Twilight Merchantiles (P) Ltd.
Ramic (1.25 mg)Tab        D.R.John & Lab
Ramicard tab                Intra Labs India Pvt Ltd
Ramichek (1.25mg)tab    Indoco Remedies Ltd
Ramihart (2.5mg)Tab       Mankind Pharmaceuticals Pvt. Ltd.
Ramil (1.25 mg) Tab        Aurobindo Pharma Ltd. (Argus)
Ramipres (10 mg) Tab     Cipla Limited
Ramipro Cap                 Emcure Pharmaceuticals
Ramiril Cap                     Micro Labs
Ramistar (10 mg)Cap      Lupin Laboratories Ltd.
Rampril (10 mg)Cap       Themis Medicare Ltd.
Ramsho (1.25 mg)Tab    Aamorb Pharmaceuticals Pvt Ltd (Xeena)
Rebeat (5 mg) Tab          Le Renon Healthcare Pvt.Ltd
Rigapril (10mg) Tab        Quadriga Biotech Pvt Ltd
RL Tab 1.25                   Sunij Pharma Pvt Ltd
Saface Tab               Morepen Laboratories Ltd.
Servace Cap               Bal Pharma (Servetus Division)
Topril Cap                     Torrent Pharmaceuticals
Variace (1.25mg) Tab    Win-Medicare Limited


PRICELIST

Odipril Hg (5 Mg) (10 Capsules in Capsule) Blue Cross Laboratories Ltd Rs. 3/Capsule Servace (5 Mg) (10 Capsules in Capsule) Servetus (Bal Pharma Limited) Rs. 3.75/Capsule Ziram (5 Mg) (10 Capsules in Capsule) FDC Limited Rs. 3.83/Capsule Ramihart (5 Mg) (7 Capsule in Capsule) Mankind Pharma Rs. 3.86/Capsule Ramm (5 Mg) (10 Capsules in Capsule) Finecure Pharmaceuticals Ltd Rs. 4.20/Capsule Rl (5 Mg) (10 Capsules in Capsule) Sunij Pharma Pvt Ltd Rs. 4.40/Capsule Acepril (5 Mg) (10 Capsules in Capsule) Sain Medicaments Pvt. Ltd Rs. 4.96/Capsule Ramidil (5 Mg) (10 Capsules in Capsule) Vazokare (Medley Pharmaceuticals Limited) Rs. 5.30/Capsule R Pril (5 Mg) (10 Capsules in Capsule) Biochem Pharmaceutical Industrial Ltd Rs. 5.40/Capsule Rampril (5 Mg) (10 Capsules in Capsule) Themis Pharmaceuticals Limited Rs. 5.60/Capsule
 

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