Drotaverine-solofarm injection 20mg / ml 2 ml ampoules 10 pcs

Description

Composition
Active substance:
1 ml of solution contains: 20 mg of drotaverine hydrochloride.
Excipients:
Ethanol 95% 67 mg, 1 mg of sodium bisulfite, water for injections to 1 mL.
Description:
Transparent or slightly opalescent liquid of light-yellow or greenish-yellow to yellow or greenish-yellow color.
Product form:
Solution for intravenous and intramuscular administration of 20 mg / ml.
In 2 ml ampoules of colored glass. 5 or 10 vials in blisters of polyvinyl chloride or polyethylene terephthalate film with a polymer film or lacquered aluminum foil or a polymer film without an aluminum foil and lacquer or in the form of cardboard with cells for stacking ampoules.
1, 5 or 10 contour of cellular packages or molds of cardboard with 10 ampoules or 1, 2, 10 or 20 contour of cellular packages or shapes from a cardboard of 5 ampoules together with instructions for use and a lancet ampulnam or without a pack of cardboard .
Contraindications
Hypersensitivity to the active substance or to any of the excipients of the formulation; hypersensitivity to sodium disulfite; severe hepatic or renal failure; severe chronic heart failure; AV-block II-III level; Children up to age 18; childbirth; lactation.
Carefully
If hypotension, atherosclerosis of the coronary arteries, prostate adenoma, glaucoma, pregnancy.
Dosage
20 mg / ml
Indications
Spasms of smooth muscle in diseases of the biliary tract: cholecystolithiasis, cholangiolithiasis, pericholecystitis, cholangitis, papillitis.
Spasms of smooth muscles of the urinary tract: nephrolithiasis, urolithiasis, pyelitis, cystitis, bladder spasm. As an adjuvant therapy (when the tablet mold can not be used): the spasms of smooth muscles of the gastrointestinal tract: gastric ulcer and duodenal ulcer, gastritis, spasm cardia, and pylorus, enteritis, colitis, spastic colitis, constipation, irritable bowel syndrome, postcholecystectomical syndrome; gynecological diseases: dysmenorrhea; during some instrumental studies, including the holetsistografii.
Interaction with other drugs
Attenuates levodopa antiparkinsonian effect (increased rigidity and tremor). Enhances (especially when administered intravenously) spasmolytic effect of papaverine, bendazol and other antispasmodics, including m-holinoblokatory. Amplifies hypotension caused by tricyclic antidepressants, quinidine, procainamide. Reduces spazmogennoe morphine activity. Phenobarbital increases the antispasmodic action Drotaverinum.
Overdose
In case of overdose may increase dose-related side effects.
Symptoms: heart block, cardiac arrest, paralysis of the respiratory center.
Treatment: In case of overdose, patients should be under close medical supervision and they should be symptomatic therapy and treatment to maintain basic bodily functions.
pharmachologic effect
Pharmacological group:
Antispasmodic.
Pharmacodynamics:
Drotaverine – isoquinoline derivative, the chemical structure and pharmacological properties similar to papaverine, but has a more pronounced and prolonged effect. Drotaverine has a strong spasmolytic effect on smooth muscle by inhibition of phosphodiesterase-4 (PDE-4). PDE4 hydrolyze cyclic adenosine monophosphate (cAMP) to adenosine monophosphate (AMP). Inhibition of PDE4 results in increased concentrations of cAMP that activates cAMP-dependent phosphorylation of myosin light chain kinase (MLCK). Phosphorylation MLCK leads to decrease its affinity for calcium ions – kalmodulinovomu complex, resulting in an inactivated form MLCK supports muscle relaxation. Cyclic adenosine monophosphate, moreover, affect the cytosolic calcium ion concentration, by stimulating the transport of calcium ions in the extracellular space and sarcoplasmic reticulum. In vitro drotaverin inhibits isozyme PDE4 isoenzymes without inhibiting PDE-3 and PDE 5, so drotaverine efficiency depends on the activity of PDE-4, which in various tissues of different content. The high content of PDE-4 noted in bile and urinary tract, the uterus, the gastrointestinal tract. Hydrolysis of cAMP in myocardial and smooth muscle of the blood vessels occurs mainly by a PDE-3, however drotaverin less influence on the cardiovascular system. Drotaverinum effective in spasms of smooth muscles of both neurogenic and muscular origin.
Pharmacokinetics:
Bioavailability – 100%. However, the system enters the bloodstream 65% of the dose (the effect of “first pass” through the liver). The time to reach maximum concentration (TCmax) – 45-60 minutes. Communication with plasma proteins – 95-97%, preferably albumin, gamma- and beta-globulin, as well as high density lipoproteins. Evenly distributed in the body, it enters the smooth muscle cells. It does not cross the blood-brain barrier. Drotaverine and / or its metabolites can slightly penetrate the placenta. Almost completely metabolized in the liver by O-dezetilirovaniya. Metabolites are rapidly conjugated with glucuronic acid. The main metabolite – 4′-dezetildrotaverin, other metabolites – 6 dezetildrotaverin and 4′-dezetildrotaveraldin. The half-life (T1 / 2) -. For 8-10 h 72 h almost completely excreted, over 50% of the kidney (primarily as metabolites) and about 30% of the intestine. Drotaverinum unchanged in the urine is detected.
Pregnancy and breast-feeding
Use of the drug during pregnancy is possible only when the intended benefits for a mother than the potential risk to the fetus. If necessary, use during breastfeeding is necessary to solve the issue of termination of breastfeeding.
Conditions of supply of pharmacies
Prescription.
side effects
Central nervous system: headache, dizziness, and insomnia.
From the cardiovascular system: tachycardia, blood pressure, arrhythmia, collapse (when administered intravenously).
From the digestive system: nausea, vomiting, constipation.
Allergic reactions: angioedema, urticaria, rash, pruritus, anaphylactic shock.
Local reactions: injection site reactions.
Other: hot flashes, sweating.
special instructions
When administered intravenously Drotaverinum in patients with low blood pressure patient should be in a horizontal position due to the risk of collapse. The preparation contains disulfite, which may cause allergic-type reactions including anaphylactic symptoms and bronchospasm in sensitized individuals, particularly in individuals with asthma or allergic diseases in history. This increased sensitivity to disulfite parenteral formulation should be avoided.
The effect on the ability of control of vehicles and mechanisms
During the period of treatment is not recommended to drive vehicles, machinery or engage in activities that require high concentration and psychomotor speed reactions.
Storage conditions
At a temperature of not higher than 25 C.
Keep out of the reach of children.
Dosing and Administration
Intramuscular injection of 2-4 ml (40-80 mg) 1-3 times a day.
The course of treatment for 1-2 weeks.
If required prolonged treatment switching to the drug in the dosage form into tablets.
In acute colic (kidney or gall stones) – 2-4 ml (40-80 mg) in 10-20 ml of 0.9% sodium chloride solution or 5% dextrose solution by slow intravenous injection (injection duration of about 30 seconds).
Not mixed in the same syringe with a solution of aminophylline.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist