Approval Date: 02/20/2007
Date of revision: 02/02/2009; 01/25/2011; 03/12/2012; 03/29/2013; 08/11/2013; 12/19/2013; 05/02/2014; 04/04/2014
Acipimox capsules instructions
Please read the instructions carefully and use under the guidance of a physician
Generic Name: Acipimox CapsulesTrade Name: Lechipine®/ OLBETAMâEnglish Name: Acipimox Capsules
Hanyu Pinyin: Aximosi Jiaonang
Ingredients
The main ingredient of this product is Acipimox, whose chemical name is: 5-methylpyrazoline-2-carboxylic acid-4 oxide
The chemical structure formula is
Molecular formula: C6H6N2O3
Molecular weight: 154.13
Properties
This product is a capsule, the content of white to yellowish powder.
Indications
This product can be used as alternative or adjuvant therapy to lower triglyceride levels in patients who are not adequately relieved by other treatments (such as statins or fibrates) for the following conditions.
Hypertriglyceridemia (Fredrickson type IV hyperlipoproteinemia)
Hypercholesterolemia and hypertriglyceridemia (Fredrickson type IIB hyperlipoproteinemia)
This product should be used only after other measures such as dietary changes and other non-pharmacological treatments (e.g., exercise, weight loss) have been taken.
The use of acipimox for the treatment of hyperlipoproteinemia has not been shown to reduce cardiovascular morbidity and mortality.
Specification】 0.25g
Dosage]
The daily dose may vary depending on plasma triglyceride and cholesterol levels. The average daily dose is: 1 capsule 2-3 times daily with meals.
Type IV hyperlipoproteinemia, 1 capsule twice daily.
For Type IIb, Type III and Type V hyperlipoproteinemia, 1 capsule 3 times daily.
The dose may be increased according to medical advice for patients with special severe conditions.
The total daily dose should not exceed 1200 mg and can be taken safely for a long time.
The dose should be adjusted according to creatinine clearance levels in patients with renal insufficiency. It can be administered as follows: one capsule daily for creatinine clearance 80-40ml/min; one capsule every other day for 40-20ml/min.
Adverse effects]
Long-term clinical treatment of a large number of patients has confirmed that the drug is well tolerated. Clinical controls and laboratory tests showed no toxic effects on major parenchymal organs and no interference with metabolic bypass (sugar and uric acid metabolism).
The drug can cause skin vasodilatation phenomena (reddening, hot flashes and itching) especially in the early stages of treatment.
These symptoms usually disappear rapidly within the first few days after treatment.
Gastrointestinal reactions (heartburn, epigastric pain), headache and malaise have occasionally been reported during treatment. Only rare cases have required discontinuation of treatment due to serious adverse reactions. Very few patients have had local and systemic reactions, sometimes severe, that may be related to immune metaplasia (e.g., rubella, eyelid and/or lip edema, rash, asthma-like dyspnea, and hypotension). Patients with these conditions should discontinue Rogaine immediately and take appropriate therapeutic measures.
The patient should inform his physician or pharmacist if any unintended reactions occur that are not mentioned in the instructions.
The following adverse reactions have been identified and reported as a result of clinical and post-marketing experience with acipimox, with the incidence defined as follows: very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1,000 to <1/100); rare (1/10,000 to <1/1,000); very rare (< 1/ 10,000); unknown (cannot be estimated from available data).
Incidence by MedDRA System Organ Classification Adverse Reactions Immune System Abnormalities Uncommon Allergic-like Reactions* Neurological Abnormalities Very Common Headache Cardiovascular System Abnormalities Very Common Flushing Unknown Vasodilation** Respiratory, Thoracic and Mediastinal Abnormalities Uncommon Bronchospasm* Gastrointestinal System Abnormalities Very Common Dyspepsia Common Epigastric Pain Uncommon Nausea* Unknown Diarrhea** Skin and Subcutaneous Tissue Abnormalities common urticaria uncommon angioedema*, pruritus*, rash*, erythema* musculoskeletal and connective tissue abnormalities uncommon myositis*, myalgia*, arthralgia* systemic abnormalities common malaise uncommon febrile sensation*, malaise** incidence of adverse reactions as assessed by postmarketing safety database
**The incidence of adverse reactions could not be assessed by the available data
Contraindications
Contraindicated in patients with hypersensitivity to the active ingredient and any excipients, in patients with peptic ulcer and in patients with severe renal impairment (creatinine clearance less than 30 ml/min).
[Precautions].
Prior to treatment with acipimox, a proper diet should be used to control blood lipids, and alcohol consumption should be stopped and exercise to reduce weight to prevent obesity. Patients are recommended to receive long-term treatment with acipimox, therefore all baseline values including lipid profile should be tested prior to treatment, and lipids should be tested periodically to determine if the desired efficacy is achieved. Liver function and renal function should be monitored.
Although no fetal damage has been observed in animal studies, acipimox is contraindicated in women who are pregnant or suspected to be pregnant and in those who are breastfeeding.
The structure of acipimox is related to niacin. The risk of muscle toxicity is increased with concomitant administration of niacin with a statin (i.e., 3-hydroxy-3-methylglutaryl coenzyme A [HMG-CoA] reductase inhibitor). One study reported a higher incidence of myopathy and rhabdomyolysis in Chinese patients taking niacin plus laropiprant in combination with simvastatin compared to Caucasians.
[Effects on the ability to drive and manipulate machines].
Although no studies are available, the pharmacodynamic and overall safety information suggests that acipimox is unlikely to affect driving and the ability to operate machinery.
Pregnant women and nursing mothers
Safety during pregnancy has not been confirmed. It is not known whether acipimox can be secreted from human breast milk. As with most drugs, it is contraindicated in pregnant and lactating women.
Pediatric use】 No relevant studies are available.
Geriatric use】 No relevant studies are available.
Drug Interactions
No adverse drug interactions have been shown in patients taking concomitant hypoglycemic or anticoagulant drugs.
No interactions with other lipid-lowering drugs were observed. However, caution should be exercised when combining acipimox with statins or fibrates, as an increase in skeletal muscle events has been reported when niacin (structural analogue of acipimox) is combined with such lipid-lowering agents.
No interactions with digoxin and warfarin have been observed.
[Drug Overdose].
No cases of drug overdose have been depicted in the literature.
If toxic reactions occur, maintenance therapy and symptomatic treatment should be administered.
Clinical trials] No relevant research data are available.
Pharmacology and Toxicology
It inhibits the release of free fatty acids from adipose tissue, reduces the concentration of very low density (VLDL) and low density (LDL) lipoproteins in the blood, and lowers triglyceride and total cholesterol levels.
During treatment, leucovorin may have a beneficial effect on HDL cholesterol by increasing its levels. The improvement in lipid levels is usually seen within the first month of treatment.
Toxicological studies in various animal species have shown low acute toxicity and good systemic and gastrointestinal tolerability with long-term treatment (up to 2 years). Studies on the reproductive system have shown that the drug has no adverse effects on reproduction, embryology or lactation. The drug is not mutagenic.
Pharmacokinetics]
After oral administration, it can be absorbed completely and rapidly, and the blood concentration reaches its peak within 2 hours, with a half-life of about 2 hours. The drug does not bind to plasma proteins, is not metabolized and is excreted in the urine.
Storage】Storage below 30°C.
Package】 PVC/Aluminium foil package, 0.25g per capsule, 30 capsules per box.
Expiration date】 48 months
Execution standard】 Imported drug registration standard JX20000205
Approval number】 Imported drug registration certificate number: H20130931 【Manufacturer】 Company name: Pfizer Italia S.r.l
Business Address: 63100 Località Marino del Tronto, Ascoli Piceno, Italy
Domestic contact address: 7-13F, Block B, Minmetals Plaza, 3-7 Chaoyangmen North Street, Dongcheng District, Beijing
Postal Code: 100010
Tel: 010-85167000
Product Hotline: 800 810 0055 (from landline); 400 610 0055 (from mobile) (working hours: Monday to Friday 9:00 – 12:00; 13:00 – 18:00)