Cyclobenzaprine apollo

Transcription

1 Cyclobenzaprine apollo Cyclobenzaprine apollo Cyclobenzaprine CAS Number : Molecular Formula : C20H21N Molecular Weight : g/mol Systematic (IUPAC) : dimethyl({3-[(2e)- tricyclo[ ^{3,8}]pentadeca-1(11),3(8),4,6,9,12,14- heptaen-2-ylidene]propyl})amine Type : small molecule

2 Description Cyclobenzaprine is a skeletal muscle relaxant and a central nervous system (CNS) depressant. Cyclobenzaprine acts on the locus coeruleus where it results in increased norepinephrine release, potentially through the gamma fibers which innervate and inhibit the alpha motor neurons in the ventral horn of the spinal cord. It is structurally similar to Amitriptyline, differing by only one double bond. Categories Muscle Relaxants Skeletal Muscle Relaxants Antidepressive Agents, Tricyclic Muscle Relaxants, Central Tranquilizing Agents Taxonomy Kingdom : Organic Classes Dibenzocycloheptenes Substructures Benzene and Derivatives Aliphatic and Aryl Amines Aromatic compounds Dibenzocycloheptenes Pharmacology

3 Indication : For use as an adjunct to rest and physical therapy for relief of muscle spasm associated with acute, painful musculoskeletal conditions. Pharmacodynamics : Cyclobenzaprine, closely related to the antidepressant amitriptyline, is used as a skeletal muscle relaxant to reduce pain and tenderness and improve mobility. Unlike dantrolene, cyclobenzaprine cannot be used to treat muscle spasm secondary to cerebral or spinal cord disease. Mechanism of action : Like other tricyclic antidepressants, cyclobenzaprine exhibits anticholinergic activity, potentiation of norepinephrine, and antagonism of reserpine. Cyclobenzaprine does not directly act on the neuromuscular junction or the muscle but relieves muscle spasms through a central action, possibly at the brain stem level. Cyclobenzaprine binds to the serotonin receptor and is considered a 5-HT2 receptor antagonist that reduces muscle tone by decreasing the activity of descending serotonergic neurons. Absorption : Slowly but well absorbed after oral administration Protein binding : Very high (93%) Metabolism : Extensively metabolized (gastrointestinal and hepatic).

4 Route of elimination : Cyclobenzaprine is extensively metabolized, and is excreted primarily as glucuronides via the kidney. Half life : 18 hours (range 8-37 hours) Clearance : 0.7 L/min Toxicity : Oral mouse and rat LD50 are 338 mg/kg and 425 mg/kg respectively. Signs of overdose include agitation, coma, confusion, congestive heart failure, convulsions, dilated pupils, disturbed concentration, drowsiness, hallucinations, high or low temperature, increased heartbeats, irregular heart rhythms, muscle stiffness, overactive reflexes, severe low blood pressure, stupor, and vomiting. Affected organisms : Humans and other mammals Drug Class And Mechanisms Cyclobenzaprine is a muscle relaxant. Specifically, cyclobenzaprine relieves muscle spasm when the spasm is due to local problems, that is, in the muscle itself and not in the nerves controlling the muscles. Cyclobenzaprine has no effect on muscle function. Cyclobenzaprine seems to accomplish its beneficial effect through a complex mechanism within the nervous system, probably in the brainstem. The FDA approved cyclobenzaprine in August Dosing

5 The recommended dose of cyclobenzaprine dose is 5 or 10 mg three times daily using immediate release tablets or 15 or 30 mg once daily using extended release tablets. Drug Interactions Cyclobenzaprine is chemically related to the tricyclic class of antidepressants (for example, amitriptyline [ Elavil, Endep], nortriptyline [ Pamelor]). As such, it should not be taken with or within two weeks of any monoamine oxidase (MAO) inhibitor, for example, isocarboxazid (Marplan), phenelzine (Nardil), tranylcypromine (Parnate), and procarbazine (Matulane). High fever, convulsions, and even death can occur when these drugs are used together. Additionally, cyclobenzaprine interacts with other medications and drugs that slow the brain's processes, such as alcohol, barbiturates, benzodiazepines (for example, diazepam [Valium], lorazepam [ Ativan]), and narcotics. Why is this medication prescribed? Cyclobenzaprine, a muscle relaxant, is used with rest, physical therapy, and other measures to relax muscles and relieve pain and discomfort caused by strains, sprains, and other muscle injuries. How should this medicine be used? Cyclobenzaprine comes as a tablet and an extended release capsule to take by mouth. The tablet is usually taken two to four times a day. The extended release capsule is usually taken one or two times a day. Do not take this drug for more than 3 weeks without talking to your doctor. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to

6 explain any part you do not understand. Take cyclobenzaprine exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor. Other uses for this medicine This medication is sometimes prescribed for other uses; ask your doctor or pharmacist for more information. What special precautions should I follow? Before taking cyclobenzaprine, tell your doctor and pharmacist if you are allergic to cyclobenzaprine or any other drugs. tell your doctor and pharmacist what prescription and nonprescription drugs you are taking or have taken within the last 2 weeks, especially medications for depression, seizures, allergies, coughs, or colds; MAO inhibitors (phenelzine [Nardil], tranylcypromine [Parnate]); sedatives; sleeping pills; tranquilizers; and vitamins. tell your doctor if you have an overactive thyroid gland, heart disease, glaucoma, or difficulty urinating. tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant while taking cyclobenzaprine, call your doctor immediately. talk to your doctor about the risks and benefits of taking cyclobenzaprine if you are 65 years of age or older. Older adults should not usually take cyclobenzaprine because it is not as safe or effective as other medications that can be used to treat the same condition.

7 you should know that this drug may make you drowsy. Do not drive a car or operate machinery until you know how cyclobenzaprine affects you. remember that alcohol can add to the drowsiness caused by this drug. What should I do if I forget a 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 the missed one. What side effects can this medication cause? Cyclobenzaprine may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away: drowsiness dry mouth dizziness upset stomach If you experience any of the following symptoms, call your doctor immediately: severe skin rash swelling of the face or tongue difficulty breathing or swallowing irregular heart rate chest pain fever seizures What storage conditions are needed for this medicine?

8 Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture (not in the bathroom). Throw away any medication that is outdated or no longer needed. Talk to your pharmacist about the proper disposal of your medication. What other information should I know? Keep all appointments with your doctor. Do not let anyone else take your medication. Ask your pharmacist any questions you have about refilling your prescription. It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of emergencies. apollo asia Division APOLLO Pharmaceuticals API Manufacturers INDIA [P] Ltd. asia Division Mr.Vipin Saxena CEO Cellular: Cellular: Direct : FAX : Wireline Purchase HELPDESK:

9 Wireline Sales HELPDESK: Wireless 24x7 HELPDESK: Blackberry Pin : 32E6500D 32E C58 apollo@hotmail.co.in Sales@apollopharma.in Export@apollopharma.in purchase@apollopharma.in Chat: MSN Hotmail:VipinrSaxena Skype NAME:VipinrSaxena Rocketmail:VipinrSaxena Google mail:vipinrsaxena BlackBerry:28415C58 Regd. Office :- 1104, Maker Chamber V, Nariman Point Mumbai, INDIA Pin: Industrial Office D-62, OIC India Oshiwara Industrial Centre,

10 New Link Road, Goregoan West, Mumbai, INDIA Pin: Manufacturing Unit Address: Plot No. 117A, Village: Chamble Near MonaTona Limited.Wada, Maharashtra, PIN : INDIA apollo@hotmail.co.in Sales@apollopharma.in Export@apollopharma.in purchase@apollopharma.in

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