Generic Name:ambenonium(discontinued drug)
Brand Name:Mytelase
Drug Class:Cholinesterase Inhibitors
What is ambenonium, and what is it used for?
Ambenonium is a medication used in the treatment ofmyasthenia gravis, an autoimmune neuromuscular disease. Myasthenia gravis affects motor nerve function causingweaknessin the skeletal muscles, which results in weakness of arms and legs, and difficulties with eye andeyelidmovement, talking, chewing, swallowing, facial expressions andbreathing. Ambenonium improves the symptoms of myasthenia gravis by enhancing the transmission of nerve signals to the muscles.
Acetylcholine is a natural chemical (neurotransmitter) that nerve endings in muscles secrete to stimulate muscle contraction. Acetylcholine stimulates protein molecules known as cholinergic receptors in the neuromuscular junctions making the muscle fibers contract. There are two types of cholinergic receptors, muscarinic and nicotinic, with diverse functions in the body. In patients with myasthenia gravis, autoimmune antibodies form against these receptors and damage and destroy them, preventing normal neurotransmission.
Ambenonium improves nerve signaling to the muscle fibers by preventing the breakdown of acetylcholine and enhancing its bioavailability. Neurotransmitters are normally broken down and reabsorbed by the nerve cells after the completion of neurotransmission, as part of a natural process. Acetylcholine is broken down by the enzyme cholinesterase. Ambenonium blocks the activity of cholinesterase and prolongs the activity of acetylcholine.
Ambenonium was discontinued by the manufacturer on June 25, 2012 and is no longer available in the U.S.
Warnings
- Do not use ambenonium in patients with hypersensitivity to any component of the formulation.
- Do not administer routinely withatropine, because it may suppress the muscarinic symptoms of excessive gastrointestinal stimulation but the more serious symptoms of muscle twitches (fasciculation) and voluntary muscleparalysismay remain.
- Do not administer concurrently with mecamylamine or other ganglionic block agents which reduce the activity of acetylcholine.
- Do not use ambenonium concurrently with otherdrugsthat enhance acetylcholine activity, except under strict medical supervision, because the drug has more prolonged action than other antimyasthenic drugs.
- There is very little warning before overdosage of ambenonium because of a very narrow margin between the first appearance of side effects and serious toxic effects. Administer the drug with extreme care and supervision, particularly when increasing dosage.
- Use ambenonium with caution in patients with:
- Asthma
- Parkinson’s disease
- Mechanical intestinal or urinary obstruction
SLIDESHOW
See SlideshowWhat are the side effects of ambenonium?
Common side effects of ambenonium include:
- Nausea
- Vomiting
- Abdominalcramps
- Diarrhea
- Excessive salivation
- Increase in bronchial secretions
- Excessive watering of eyes (lachrymation)
- Sweating
- Excessive urination (pollakiuria)
- Urinary urgency
- Muscle twitches (fasciculation)
- Paralysis of tongue muscles
- Paralysis of respiratory muscles
- Difficulty swallowing
- Difficulty breathing
- Shortness of breath(dyspnea)
- Increase in官网地址bwin
- Slowheartrate (bradycardia)
- Constriction of pupils (miosis)
- Anxiety
- Panic
- General unwell feeling (malaise)
- Vertigo
Call your doctor immediately if you experience any of the following symptoms or serious side effects while using this drug:
- Seriousheart symptomsinclude fast or pounding heartbeats, fluttering in your chest, shortness of breath, and suddendizziness;
- Severeheadache,confusion, slurred speech, severe weakness,vomiting, loss of coordination, feeling unsteady;
- 严重的神经系统反应性病ff muscles, highfever,sweating, confusion, fast or uneven heartbeats,tremors, and feeling like you might pass out; or
- Serious eye symptoms includeblurred vision,tunnel vision,eye painor swelling, or seeing halos around lights.
This is not a complete list of all side effects or adverse reactions that may occur from the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may also report side effects or health problems to the FDA at 1-800-FDA-1088.
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What are the dosages of ambenonium?
Tablet
- 10 mg
Myasthenia Gravis
Adult:
- Initial: 5 mg orally every 6-8 hours
- Maintenance: 15-100 mg/day, usual 40 mg/day
- Up to 50-75 mg orally every 6-8 hours
Pediatric:
- Initial: 0.3 mg/kg/day divided every 6-8 hours orally
- Maintenance: 1.5 mg/kg/day divided every 6-8 hours orally
Overdose
- Symptoms of ambenonium overdose include increased gastrointestinal stimulation with epigastric distress, abdominal cramps, vomiting,diarrheaand excessive salivation, excessive urination, urinary urgency,coldsweats, constriction of pupils, blurred vision, respiratory and swallowing difficulty, muscle twitches and paralysis of voluntary muscles.
- Overdose treatment includes discontinuation of ambenonium, administration of atropine to reverse acetylcholine effects on the muscarinic receptors and pralidoxime chloride to reverse its effects on the nicotinic receptors. Other supportive treatments such as oxygen and artificialrespirationmay be used as required.
What drugs interact with ambenonium?
Inform your doctor of all medications you are currently taking, who can advise you on any possibledrug interactions. Never begin taking, suddenly discontinue, or change the dosage of any medication without your doctor’s recommendation.
- Ambenonium has no listed severe, serious, moderate, or mild interactions with other drugs.
The drug interactions listed above are not all of the possible interactions or adverse effects. For more information on drug interactions, visit the RxList Drug Interaction Checker.
It is important to always tell your doctor, pharmacist, or health care provider of all prescription andover-the-countermedications you use, as well as the dosage for each, and keep a list of the information. Check with your doctor or health care provider if you have any questions about the medication.
Pregnancy and breastfeeding
- The safety of ambenonium use inpregnantwomen has not been established. Ambenonium should be used in women who are pregnant or havepregnancypotential only if clearly needed, and if maternal benefits outweigh potential risks to the fetus.
- It is not known if ambenonium is present in breastmilk, but it is likely because many drugs are excreted in breastmilk. Decision to discontinue the drug ornursingshould be made depending on the mother’s clinical need, because of the potential for serious adverse reactions in thebreastfedinfant.
What else should I know about ambenonium?
- Take ambenonium exactly as prescribed.
- Store safely out of reach of children.
- In case of overdose, seek immediate medical help or contactPoison Control.
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Summary
Ambenonium is a discontinued prescription drug used to treat myasthenia gravis, an autoimmune neuromuscular disease. Ambenonium should be used with caution in people with asthma, Parkinson’s disease, and mechanical intestinal or urinary obstruction. Common side effects of ambenonium include nausea, vomiting, abdominal cramps, diarrhea, excessive salivation, increase in bronchial secretions, excessive watering of eyes (lachrymation), sweating, excessive urination (pollakiuria), urinary urgency, muscle twitches (fasciculation), paralyzed tongue muscles, paralyzed respiratory muscles, difficulty swallowing, difficulty breathing, shortness of breath (dyspnea), and others.
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Report Problems to the Food and Drug Administration
You are encouraged to report negative side effects of prescription drugs to the FDA. Visit theFDA MedWatchwebsite or call 1-800-FDA-1088.
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/010155s022lbl.pdf
https://pubchem.ncbi.nlm.nih.gov/compound/Ambenonium
https://go.drugbank.com/drugs/DB01122
https://www.ninds.nih.gov/health-information/disorders/myasthenia-gravis