Consists of Caffeine, Chlorphenamine, Ergotamine, Metamizole, Metoclopramide
What is Caffeine?
Caffeine is a central nervous system stimulant. It works by stimulating the brain. Caffeine is found naturally in foods and beverages such as coffee, tea, colas, energy and chocolate. Botanical sources of caffeine include kola nuts, guarana, and yerba mate. Caffeine is also available in prescription and non-prescription medications.
Caffeine is used to restore mental alertness or wakefulness during fatigue or drowsiness. Caffeine is also found in some headache and migraine medications, in certain dietary supplements used for weight loss, and in many popular energy drinks.
Caffeine (Caffeine) is available by prescription only. It is used for short-term treatment of neonatal apnea (breathing problems).
Caffeine may also be used for other conditions as determined by your health care provider.
Caffeine indications
Caffeine and Sodium Benzoate Injection has been used in conjunction with supportive measure to treat respiratory depression associated with overdosage with CNS depressant drugs (e.g., narcotic analgesics, alcohol). However, because of questionable benefit and transient action, most authorities believe caffeine and other analeptics should not be used in these conditions and recommend other supportive therapy.
How should I use Caffeine?
Use caffeine as directed by your health care provider. If the medication is OTC, check the label on the bottle for the exact dosing instructions. If you have any questions about the use of an OTC medication, ask your pharmacist.
- Caffeine may be taken with or without food. If caffeine upsets your stomach, take it with food.
- Do not exceed the recommended dose of caffeine. Caffeine can be habit-forming.
- Most OTC medications used for mental alertness contain 200 milligrams of caffeine per tablet or capsule. The usual maximum recommended dose of OTC caffeine is no more than 200 mg every 3-4 hours, or 1600 mg per day.
- Do not double-up on your caffeine dose if you should miss the time for next dose.
- The average cup of coffee contains 150-200 milligrams (mg) of caffeine per cup, while a cup of tea will have about 60 mg of caffeine. Cola products have about 30-40 mg of caffeine, and most energy drinks have about 60-70 mg. Be sure to account for any dietary caffeine that is consumed.
Ask your health care provider any questions you may have about how to use caffeine.
Uses of Caffeine in details
Use: Labeled Indications
Caffeine: Treatment of idiopathic apnea of prematurity
Caffeine and sodium benzoate: See Off-Label uses.
Caffeine [OTC labeling]: Restore mental alertness or wakefulness when experiencing fatigue
Off Label Uses
Augmentation of seizure induction during electroconvulsive therapy (caffeine and sodium benzoate)
Data from a randomized, double blind study as well as a few unblinded studies support the use of caffeine/sodium benzoate in the treatment of augmentation of seizure induction during electroconvulsive therapy (ECT).
Caffeine description
A methylxanthine naturally occurring in some beverages and also used as a pharmacological agent. Caffeine's most notable pharmacological effect is as a central nervous system stimulant, increasing alertness and producing agitation. It also relaxes smooth muscle, stimulates cardiac muscle, stimulates diuresis, and appears to be useful in the treatment of some types of headache. Several cellular actions of caffeine have been observed, but it is not entirely clear how each contributes to its pharmacological profile. Among the most important are inhibition of cyclic nucleotide phosphodiesterases, antagonism of adenosine receptors, and modulation of intracellular calcium handling. [PubChem]
Caffeine dosage
Usual Adult Dose for Drowsiness:
100 to 200 mg orally not more often than every 3 to 4 hours.
For occasional use only.
Not intended for use as a substitute for sleep.
Limit the use of caffeine containing medications, foods, or beverages while taking this product because too much caffeine may cause nervousness, irritability, sleeplessness, and occasionally, rapid heartbeat.
Usual Pediatric Dose for Drowsiness:
>= 12 years: 100 to 200 mg not more often than every 3 to 4 hours.
For occasional use only.
Not intended for use as a substitute for sleep.
Limit the use of caffeine containing medications, foods, or beverages while taking this product because too much caffeine may cause nervousness, irritability, sleeplessness, and occasionally, rapid heartbeat.
Usual Pediatric Dose for Apnea of Prematurity:
For short term treatment of apnea of prematurity in infants between 28 and <33 weeks gestational age.
Prior to initiation of Caffeine, baseline serum levels of caffeine should be measured in infants previously treated with theophylline, since preterm infants metabolize theophylline to caffeine. Likewise, baseline serum levels of caffeine should be measured in infants born to mothers who consumed caffeine prior to delivery, since caffeine readily crosses the placenta.
Loading Dose: 20 mg/kg Caffeine intravenous (over 30 minutes) once
Maintenance Dose: 5 mg/kg Caffeine intravenous (over 10 minutes) or orally every 24 hours.
Note: The dose of caffeine base is one-half the dose when expressed as Caffeine (e.g., 20 mg of Caffeine is equivalent to 10 mg of caffeine base).
Serum concentrations of caffeine may need to be monitored periodically throughout treatment to avoid toxicity. Serious toxicity has been associated with serum levels greater than 50 mg/L.
Apnea of prematurity is a diagnosis of exclusion. Other causes of apnea (e.g., central nervous system disorders, primary lung disease, anemia, sepsis, metabolic disturbances, cardiovascular abnormalities, or obstructive apnea) should be ruled out or properly treated prior to initiation of Caffeine.
Caffeine should be used with caution in infants with seizure disorders or cardiovascular disease.
The duration of treatment of apnea of prematurity in the placebo-controlled trial was limited to 10 to 12 days. The safety and efficacy of Caffeine for longer periods of treatment have not been established.
Caffeine interactions
See also:
What other drugs will affect Caffeine?
Acebrophylline: May enhance the stimulatory effect of CNS Stimulants. Avoid combination
Adenosine: Caffeine and Caffeine Containing Products may diminish the therapeutic effect of Adenosine. Management: Monitor for decreased effect of adenosine if patient is receiving caffeine. Discontinue caffeine in advance of scheduled diagnostic use of adenosine whenever possible. Consider therapy modification
Amifampridine: Agents With Seizure Threshold Lowering Potential may enhance the neuroexcitatory and/or seizure-potentiating effect of Amifampridine. Monitor therapy
AtoMOXetine: May enhance the hypertensive effect of Sympathomimetics. AtoMOXetine may enhance the tachycardic effect of Sympathomimetics. Monitor therapy
Broccoli: May decrease the serum concentration of CYP1A2 Substrates (High risk with Inducers). Monitor therapy
Bromperidol: Caffeine and Caffeine Containing Products may decrease the absorption of Bromperidol. Monitor therapy
BuPROPion: May enhance the neuroexcitatory and/or seizure-potentiating effect of Agents With Seizure Threshold Lowering Potential. Monitor therapy
Cannabinoid-Containing Products: May enhance the tachycardic effect of Sympathomimetics. Exceptions: Cannabidiol. Monitor therapy
Cannabis: May decrease the serum concentration of CYP1A2 Substrates (High risk with Inducers). Monitor therapy
CloZAPine: CYP1A2 Inhibitors (Weak) may increase the serum concentration of CloZAPine. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs. Monitor therapy
Cocaine (Topical): May enhance the hypertensive effect of Sympathomimetics. Management: Consider alternatives to use of this combination when possible. Monitor closely for substantially increased blood pressure or heart rate and for any evidence of myocardial ischemia with concurrent use. Consider therapy modification
CYP1A2 Inducers (Moderate): May decrease the serum concentration of Caffeine and Caffeine Containing Products. Monitor therapy
CYP1A2 Inhibitors (Moderate): May increase the serum concentration of Caffeine and Caffeine Containing Products. Monitor therapy
CYP1A2 Inhibitors (Strong): May increase the serum concentration of Caffeine and Caffeine Containing Products. Monitor therapy
Doxofylline: Caffeine and Caffeine Containing Products may enhance the adverse/toxic effect of Doxofylline. Avoid combination
Esketamine: May enhance the hypertensive effect of CNS Stimulants. Monitor therapy
Formoterol: Caffeine and Caffeine Containing Products may enhance the adverse/toxic effect of Formoterol. Caffeine and Caffeine Containing Products may enhance the hypokalemic effect of Formoterol. Monitor therapy
Guanethidine: May enhance the arrhythmogenic effect of Sympathomimetics. Guanethidine may enhance the hypertensive effect of Sympathomimetics. Monitor therapy
Indacaterol: Caffeine and Caffeine Containing Products may enhance the adverse/toxic effect of Indacaterol. Caffeine and Caffeine Containing Products may enhance the hypokalemic effect of Indacaterol. Monitor therapy
Iohexol: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Iohexol. Specifically, the risk for seizures may be increased. Management: Discontinue agents that may lower the seizure threshold 48 hours prior to intrathecal use of iohexol. Wait at least 24 hours after the procedure to resume such agents. In nonelective procedures, consider use of prophylactic anticonvulsants. Consider therapy modification
Iomeprol: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Iomeprol. Specifically, the risk for seizures may be increased. Management: Discontinue agents that may lower the seizure threshold 48 hours prior to intrathecal use of iomeprol. Wait at least 24 hours after the procedure to resume such agents. In nonelective procedures, consider use of prophylactic anticonvulsants. Consider therapy modification
Iopamidol: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Iopamidol. Specifically, the risk for seizures may be increased. Management: Discontinue agents that may lower the seizure threshold 48 hours prior to intrathecal use of iopamidol. Wait at least 24 hours after the procedure to resume such agents. In nonelective procedures, consider use of prophylactic anticonvulsants. Consider therapy modification
Linezolid: May enhance the hypertensive effect of Sympathomimetics. Management: Reduce initial doses of sympathomimetic agents, and closely monitor for enhanced pressor response, in patients receiving linezolid. Specific dose adjustment recommendations are not presently available. Consider therapy modification
Lithium: Caffeine and Caffeine Containing Products may decrease the serum concentration of Lithium. Monitor therapy
Norfloxacin: May increase the serum concentration of Caffeine and Caffeine Containing Products. Monitor therapy
Olodaterol: Caffeine and Caffeine Containing Products may enhance the adverse/toxic effect of Olodaterol. Caffeine and Caffeine Containing Products may enhance the hypokalemic effect of Olodaterol. Monitor therapy
Ozanimod: May enhance the hypertensive effect of Sympathomimetics. Management: Concomitant use of ozanimod with sympathomimetic agents is not recommended. If combined, monitor patients closely for the development of hypertension, including hypertensive crises. Consider therapy modification
Pipemidic Acid: May increase the serum concentration of Caffeine and Caffeine Containing Products. Monitor therapy
Regadenoson: Caffeine and Caffeine Containing Products may diminish the vasodilatory effect of Regadenoson. Management: Avoiding using caffeine or other methylxanthine containing products (e.g., theophylline) for at least 12 hours prior to the administration of regadenoson. Consider therapy modification
Solriamfetol: Sympathomimetics may enhance the hypertensive effect of Solriamfetol. Sympathomimetics may enhance the tachycardic effect of Solriamfetol. Monitor therapy
Solriamfetol: CNS Stimulants may enhance the hypertensive effect of Solriamfetol. CNS Stimulants may enhance the tachycardic effect of Solriamfetol. Monitor therapy
Stiripentol: May increase the serum concentration of Caffeine and Caffeine Containing Products. Avoid combination
Sympathomimetics: May enhance the adverse/toxic effect of other Sympathomimetics. Monitor therapy
Tedizolid: May enhance the hypertensive effect of Sympathomimetics. Tedizolid may enhance the tachycardic effect of Sympathomimetics. Monitor therapy
Theophylline Derivatives: CYP1A2 Inhibitors (Weak) may increase the serum concentration of Theophylline Derivatives. Exceptions: Dyphylline. Monitor therapy
TiZANidine: CYP1A2 Inhibitors (Weak) may increase the serum concentration of TiZANidine. Management: Avoid these combinations when possible. If combined use is necessary, initiate tizanidine at an adult dose of 2 mg and increase in 2 to 4 mg increments based on patient response. Monitor for increased effects of tizanidine, including adverse reactions. Consider therapy modification
Tobacco (Smoked): May decrease the serum concentration of Caffeine and Caffeine Containing Products. Monitor therapy
Caffeine side effects
See also:
What are the possible side effects of Caffeine?
Cardiovascular
Tachycardia; extrasystoles; palpitations; other cardiac arrhythmias.
CNS
Insomnia; restlessness; excitement; nervousness; tinnitus; scintillating scotoma; muscular tremor; headache; lightheadedness.
Dermatologic
Urticaria; rash, dry skin, skin breakdown (Caffeine).
EENT
Retinopathy of prematurity (Caffeine).
GI
Vomiting; nausea; diarrhea; stomach pain; necrotizing enterocolitis, gastritis, GI hemorrhage (Caffeine).
Genitourinary
Diuresis; kidney failure (Caffeine).
Hematologic
Disseminated intravascular coagulation (Caffeine).
Metabolic
Hyperglycemia; acidosis (Caffeine).
Respiratory
Dyspnea, lung edema (Caffeine).
Miscellaneous
Hypersensitivity (eg, dermatitis, rhinitis, bronchial asthma); feeding intolerance, sepsis, accidental injury, hemorrhage, cerebral hemorrhage (Caffeine).
Caffeine contraindications
See also:
What is the most important information I should know about Caffeine?
Caffeine should not be given to a child who has had an allergic reaction to it in the past.
Before using Caffeine, tell the doctor if your child is allergic to any drugs, or has a seizure disorder, heart disease, kidney disease, liver disease, or high or low blood sugar.
Do not use the medication for longer than 12 days without the advice of your child's doctor.
Each bottle of Caffeine is for one use only, even if your child does not use the entire bottle for a single dose. Throw away any medication left over in the bottle after measuring your child's dose.
Call your doctor if the child's breathing symptoms do not improve after using Caffeine.
To be sure Caffeine is helping your child's condition, the child's blood will need to be tested on a regular basis. Do not miss any scheduled appointments.
Chlorphenamine indications
Infectious-inflammatory diseases caused by microorganisms susceptible to ciprofloxacin, including respiratory diseases, diseases of abdominal and pelvic organs, bones, joints, skin, septicemia; severe infections of ENT organs. Treatment of postoperative infections. Prevention and treatment of infections in patients with reduced immunity.
For Chlorphenamine Citadel Fine Pharmaceuticals local use: acute and subacute conjunctivitis, blepharoconjunctivitis, blepharitis, bacterial corneal ulcers, keratitis, keratoconjunctivitis, chronic dacryocystitis, meybomity. Infectious lesions in the eyes from injury or contact with foreign bodies. Preoperative prophylaxis in ophthalmic surgery.
Chlorphenamine description
A histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma. It has also been used in veterinary applications. One of the most widely used of the classical antihistaminics, it generally causes less drowsiness and sedation than promethazine. [PubChem]
Chlorphenamine dosage
Individual. For oral administration dose of Chlorphenamine Citadel Fine Pharmaceuticals is 250-750 mg 2 times / day. Treatment duration is from 7-10 days to 4 weeks.
For IV administration a single dose is 200-400 mg, the multiplicity of the introduction is 2 times / day, duration of treatment - 1-2 weeks and more if necessary. May be IV injected as jet but more preferably a drip for 30 minutes.
When Chlorphenamine Citadel Fine Pharmaceuticals applied topically instilled 1-2 drops into the lower conjunctival sac of the affected eye every 1-4 hours. After improving the intervals between instillation can be increased. The maximum oral daily dose for adults is 1.5 g.
Chlorphenamine interactions
Activity increases when combined with beta-lactam antibiotics, aminoglycosides, vancomycin, clindamycin, metronidazole. Sukralfat, bismuth preparations, antacids containing aluminum ions, magnesium or calcium, cimetidine, ranitidine, vitamin and mineral supplement, iron sulfate, zinc, didanosine (recommended for 2 hours before or 4 hours after these drugs) reduce the suction. Probenecid, azlocillin increase the concentration in the blood. Decreases clearance and increases in plasma Chlorphenamine, aminophylline and theophylline (increased likelihood of side effects). Chlorphenamine Citadel Fine Pharmaceuticals enhances the effect of warfarin and other oral anticoagulants (prolongs bleeding time). Increases nephrotoxicity of cyclosporine, increase the risk of CNS excitability and convulsive reactions against the background of NSAIDs. Medicines alkalinizing the urine (citrates, sodium bicarbonate, carbonic anhydrase inhibitors) reduce the solubility (increases the probability of crystalluria). Infusion solutions of ciprofloxacin ready to use can be combined with infusion solutions: 0.9% sodium chloride solution, Ringer's solution, Ringer lactate, 5 and 10% dextrose, 10% solution of fructose, and a solution containing 5% dextrose with 0,225 or 0.45% sodium chloride. Incompatible with solutions having a pH > 7.
Chlorphenamine side effects
Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.
Check with your doctor as soon as possible if any of the following side effects occur:
Rare
Fever
skin rash or itching
sore throat and fever
unusual tiredness and weakness
Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:
Less common
Abdominal or stomach pain or upset
diarrhea
nausea or vomiting
Rare
Dizziness
hair loss
headache
Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.
Chlorphenamine contraindications
Injection: Chlorphenamine is contraindicated in comatose states, in patients who have received large amounts of central-nervous-system depressants (alcohol, sedative hypnotics, including barbiturates, general anesthetics, narcotics, narcotic analgesics, tranquilizers, etc.), and in patients who have demonstrated an idiosyncrasy or hypersensitivity to promethazine.
Under no circumstances should promethazine be given by intra-arterial injection due to the likelihood of severe arteriospasm and the possibility of resultant gangrene
Chlorphenamine HCl injection should not be given by the subcutaneous route; evidence of chemical irritation has been noted, and necrotic lesions have resulted on rare occasions following subcutaneous injection. The preferred parenteral route of administration is by deep intramuscular injection.
Syrup, Tablets and Suppositories: Phenergan Tablets and Suppositories are contraindicated for use in pediatric patients less than two years of age.
Phenergan Tablets and Suppositories are contraindicated in comatose states, and in individuals known to be hypersensitive or to have had an idiosyncratic reaction to promethazine or to other phenothiazines.
Antihistamines are contraindicated for use in the treatment of lower respiratory tract symptoms including asthma.
What is Ergotamine?
Ergotamine is in a group of drugs called ergot alkaloids (ER-got AL-ka-loids). It works by narrowing the blood vessels around the brain. Ergotamine also affects blood flow patterns that are associated with certain types of headaches.
Ergotamine is used to treat a migraine type headache.
This medication will only treat a headache that has already begun. It will not prevent migraine headaches or reduce the number of attacks.
Ergotamine should not be used to treat common tension headaches or any headache that seems to be different from your usual migraine headaches.
Ergotamine may also be used for purposes not listed in this medication guide.
Ergotamine indications
Sublingual
Migraine
Adult: As ergotamine tartrate: 2 mg on the onset of attack, then 2 mg every 30 min if necessary. Max: 6 mg/24 hr, 10 mg/wk.
Renal impairment: Contraindicated.
Hepatic impairment: Contraindicated.
Inhalation
Migraine
Adult: As ergotamine tartrate: Inhale single dose (360 mcg) at the onset of attack and repeat at 5-min intervals, if necessary. Max: 6 inhalations/24 hr, 15 inhalations/wk.
Renal impairment: Contraindicated.
Hepatic impairment: Contraindicated.
How should I use Ergotamine?
Use ergotamine as directed by your doctor. Check the label on the medicine for exact dosing instructions.
- Take ergotamine at the first sign of a migraine attack as directed by your doctor.
- Do not swallow, crush, or chew sublingual tablets. Place the tablet under your tongue and allow it to slowly dissolve. Do not eat, drink, or smoke while the tablet is dissolving.
- If you need more than 1 dose of ergotamine to treat a migraine attack, take the second dose at least 30 minutes after the first dose. Do not take more than 2 tablets for any migraine attack.
- Do not take more than 3 tablets in a 24 hour period. Do not take more than 5 tablets within a 7 day period, unless otherwise directed by your doctor.
- Do not use ergotamine daily on a regular basis.
- Check with your doctor before including grapefruit or grapefruit juice in your diet while you take ergotamine.
- If you miss a dose of ergotamine and you still have a headache, follow your doctor's dosing instructions. Contact your doctor immediately if you are unsure of what to do if you miss a dose. Do not take ergotamine more often than prescribed. Do not take 2 doses at once.
Ask your health care provider any questions you may have about how to use ergotamine.
Uses of Ergotamine in details
Ergotamine is used (usually in combination with Ergotamine and cyclizine) to relieve the symptoms of a migraine attack.
Ergotamine description
A vasoconstrictor found in ergot of Central Europe. It is an alpha-1 selective adrenergic agonist and is commonly used in the treatment of migraine disorders. [PubChem]
Ergotamine dosage
Procedure
For best results, dosage should start at the first sign of an attack. Early Administration Gives Maximum Effectiveness. At the first sign of an attack or to relieve symptoms after onset of an attack, one 2 mg tablet is placed under the tongue. Another tablet should be taken at half-hour intervals thereafter, if necessary, but dosage must not exceed three tablets in any 24hour period. Total weekly dosage should not exceed five tablets (10 mg) in any one week. Ergotamine (ergotamine tartrate tablets) ® Sublingual Tablets should not be used for chronic daily administration.
How supplied
Ergotamine® Sublingual Tablets, 2 mg
(ergotamine tartrate tablets USP)
Ergotamine (ergotamine tartrate tablets) ® Sublingual Tablets are round, green tablets each containing 2 mg of ergotamine tartrate. They are debossed with the product identification code "LB2" on one side, and are supplied in individual foil strips packaged in a plastic child resistant canister containing 20 tablets (5 - 2 x 2 foil strips) NDC 10802-1202-0
Store and Dispense
Store at 20°- 25°C (68° - 77°F); excursions permitted to 15° - 30°C (59° - 86°F). Protect from light and heat. Keep out of reach of children.
Manufactured for: Rosedale Therapeutics Bristol, TN 37620 USA. By: Mikart, Inc. Atlanta, GA 30318. Rev 08/2007. FDA rev date: 6/30/1995
Ergotamine interactions
See also:
What other drugs will affect Ergotamine?
CYP 3A4 Inhibitors (e.g. Macrolide Antibiotics and Protease inhibitors)
Ergotamine® Sublingual Tablets (ergotamine tartrate tablets USP) should not be administered with other vasoconstrictors. Use with sympathomimetics (pressor agents) may cause extreme elevation of blood pressure. The beta-blocker lnderal (propranolol) has been reported to potentiate the vasoconstrictive action of ergotamine by blocking the vasodilating property of epinephrine. Nicotine may provoke vasoconstriction in some patients, predisposing to a greater ischemic response to ergot therapy. The blood levels of ergotamine-containing drugs are reported to be elevated by the concomitant administration of macrolide antibiotics and vasospastic reactions have been reported with therapeutic doses of the ergotamine-containing drugs when coadministered with these antibiotics.
Ergotamine side effects
See also:
What are the possible side effects of Ergotamine?
Cardiovascular: Vasoconstrictive complications of a serious nature may occur at times. These include ischemia, cyanosis, absence of pulse, cold extremities, gangrene, precordial distress and pain, EKG changes and muscle pains. Although these effects occur most commonly with long-term therapy at relatively high doses, they have also been reported with short-term or normal doses. Other cardiovascular adverse effects include transient tachycardia or bradycardia and hypertension.
Gastrointestinal: Nausea and vomiting
Neurological: paresthesias, numbness, weakness, and vertigo.
Allergic: Localized edema and itching.
Fibrotic Complications:.
Drug Abuse and Dependence
There have been reports of drug abuse and psychological dependence in patients on ergotamine tartrate therapy. Due to the chronicity of vascular headaches, it is imperative that patients be advised not to exceed recommended dosages with long-term use to avoid ergotism.
Ergotamine contraindications
See also:
What is the most important information I should know about Ergotamine?
Coadministration of ergotamine with potent CYP 3A4 inhibitors (ritonavir, nelfinavir, indinavir, erythromycin, clorithromycin and troleandomycin) has been associated with acute ergot toxicity (ergotism) characterized by vasospasm and ischemia of the extremities, with some cases resulting in amputation. There have been rare reports of cerebral ischemia in patients on protease inhibitor therapy when ergotamine was coadministered, at least one resulting in death. Because of the increased risk for ergotism and other serious vasospastic adverse events, ergotamine use is contraindicated with these drugs and other potent inhibitors of CYP 3A4 (e.g., ketoconazole, itraconazole).
Ergotamine (ergotamine tartrate tablets) ® Sublingual Tablets may cause fetal harm when administered to pregnant women. Ergotamine (ergotamine tartrate tablets) ® Sublingual Tablets are contraindicated in women who are or may become pregnant. If this drug is used during pregnancy or if the patient becomes pregnant while taking this product, the patient should be apprised of the potential hazard to the fetus. Peripheral vascular disease, coronary heart disease, hypertension, impaired hepatic or renal function and sepsis.
Hypersensitivity to any of the components.
Metamizole indications
Metamizole tablets are used for the treatment of pains of different origin and variable intensity: toothache, headache, arthralgia, neuralgia, myositis, mild to moderate visceral pain, high fever, not responding to other drugs.
Uses of Metamizole in details
Metamizole is used to treat pain of different origins such as toothache, headache, visceral pain or high fever. It is also used to treat severe pain associated with surgeries, cancer or stomach problems.
Metamizole description
A thioureylene antithyroid agent that inhibits the formation of thyroid hormones by interfering with the incorporation of iodine into tyrosyl residues of thyroglobulin. This is done by interfering with the oxidation of iodide ion and iodotyrosyl groups through inhibition of the peroxidase enzyme.
Metamizole dosage
The dosing regimen of Metamizole is individual. When this medication is administered orally of the single dose is 20-40 mg. The daily dose is 20-80 mg, the frequency of use is 1-2 times / day. The duration of treatment is 2-8 weeks.
Metamizole interactions
Metamizole potentiates the analgesic and antipyretic action of the nonsteroidal antiinflammatory drugs. The Metamizole effects are potentiated by the tricyclic antidepressants, oral contraceptive agents, allopurinol, alcohol. Metamizole decreases the activity of the coumarin anticoagulants and plasma levels of cyclosporin. The enzyme inductors (barbiturates, glutethimide, phenylbutazone) attenuate the Metamizole effects. Metamizole potentiates the effects of the drugs possessing CNS depressant activity. Concurrent administration with chlorpromazine is related with a risk of severe hypothermia. Metamizole can be used in combination with buscolysin, atropin, codein.
Metamizole side effects
May be nausea, vomiting, diarrhea or constipation, urticaria, hypersensitivity to the drug. Rarely granulocytopenia, epigastric pain, stomatitis. Regardless of the dose, Metamizole magnesium (Metamizole) can occasionally determine hypersensitivity, externalized, such as rash, leukopenia and rarely agranulocytosis, as well as fragments of impact or shock. Presented unfamiliar or unpleasant sensations impaired skin and mucous membranes, will need to stop and seek medical preparations.
If it had been observed previously and phenomena of intolerance to other analgesics or anti-flu preparations, consult your doctor before applying Metamizole magnesium (Metamizole). After intravenous injection, there may be dizziness, feeling of oppression and demonstrations by the CNS, without allergic genesis. After intravenous injection, there may be dizziness, feeling of oppression and demonstrations by the CNS, without allergic genesis. These side effects are largely avoided by slow injection (1 to 1.5 ml per minute). Rarely, injection Metamizole magnesium (Metamizole), depending on the dose may lead to hypotension, without hypersensitivity reactions.
Metamizole contraindications
Active gastroduodenal ulcer, liver failure, hepatitis, nephritis, blood dyscrasias, cardiac failure, oliguria. Do not be administered for prolonged periods. Metamizole magnesium (Metamizole) has not administered in case of allergy to pyrazolone (eg, hypersensitivity to drugs with Metamizole magnesium, isopirina, propyphenazone, phenazone or phenylbutazone), and certain metabolic disorders (hepatic porphyria, congenital deficiency of glucose-6-phosphate dehydrogenase), patients with hypersensitivity to analgesics (pain relievers asthma) infants during the first three months and less than 5 kg of weight, patients with blood pressure below 100 mm Hg or movement unstable hematopoiesis and injured patients.
What is Metoclopramide?
Metoclopramide is used to treat the symptoms of a certain type of stomach problem called gastroparesis in patients with diabetes. It works by increasing the movements or contractions of the stomach and intestines. It relieves symptoms such as nausea, vomiting, heartburn, a feeling of fullness after meals, and loss of appetite. Metoclopramide is also used to treat heartburn for patients with gastroesophageal reflux disease (GERD). GERD is esophageal irritation from the backward flow of gastric acid into the esophagus.
metoclopramide is available only with your doctor's prescription.
Once a medicine has been approved for marketing for a certain use, experience may show that it is also useful for other medical problems. Although these uses are not included in product labeling, metoclopramide is used in certain patients with the following medical conditions:
- Failure of the stomach to empty its contents.
- Nausea and vomiting caused by other medicines.
- Persistent hiccups.
- Prevention of aspirating fluid into the lungs during surgery.
- Vascular headaches.
Metoclopramide indications
The use of Metoclopramide™ (Metoclopramide) is recommended for adults only. Therapy should not exceed 12 weeks in duration.
Symptomatic Gastroesophageal Reflux
Metoclopramide™ (Metoclopramide) is indicated as short-term (4 to 12 weeks) therapy for adults with symptomatic, documented gastroesophageal reflux who fail to respond to conventional therapy.
The principal effect of metoclopramide is on symptoms of postprandial and daytime heartburn with less observed effect on nocturnal symptoms. If symptoms are confined to particular situations, such as following the evening meal, use of metoclopramide as single doses prior to the provocative situation should be considered, rather than using the drug throughout the day. Healing of esophageal ulcers and erosions has been endoscopically demonstrated at the end of a 12-week trial using doses of 15 mg four times daily. As there is no documented correlation between symptoms and healing of esophageal lesions, patients with documented lesions should be monitored endoscopically.
Diabetic Gastroparesis (Diabetic Gastric Stasis)
Metoclopramide™ (Metoclopramide) is indicated for the relief of symptoms associated with acute and recurrent diabetic gastric stasis. The usual manifestations of delayed gastric emptying (e.g., nausea, vomiting, heartburn, persistent fullness after meals, and anorexia) appear to respond to metoclopramide within different time intervals.
Important Limitations
Metoclopramide™ (Metoclopramide) is indicated for adults only. Therapy should not exceed 12 weeks in duration. The safety and effectiveness in pediatric patients have not been established.
How should I use Metoclopramide?
Use Metoclopramide as directed by your doctor. Check the label on the medicine for exact dosing instructions.
- Metoclopramide comes with an extra patient information sheet called a Medication Guide. Read it carefully. Read it again each time you get Metoclopramide refilled.
- Take Metoclopramide by mouth 30 minutes before meals and at bedtime without food or water unless directed otherwise by your doctor.
- Do not remove the tablet from the blister pack until you are ready to take Metoclopramide. Make sure that your hands are dry when you open the blister pack. If the tablet breaks or crumbles while handling, discard and remove a new tablet. Place the tablet on your tongue. The tablet dissolves quickly and can be swallowed with saliva. Take the tablet immediately after opening the blister pack. Do not store the removed tablet for future use.
- It may take several days to weeks for Metoclopramide to work. Do not stop taking Metoclopramide without checking with your doctor.
- If you miss a dose of Metoclopramide, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once.
Ask your health care provider any questions you may have about how to use Metoclopramide.
Uses of Metoclopramide in details
Use: Labeled Indications
Injection:
Chemotherapy-induced nausea and vomiting, prophylaxis: Prophylaxis of nausea and vomiting associated with emetogenic cancer chemotherapy. Note: Injectable metoclopramide prior to moderate- to high-emetic-risk chemotherapy is rarely indicated due to the potential for neurologic events and availability of more efficacious alternative agents.
Gastroparesis, diabetic: Relief of symptoms associated with acute and recurrent diabetic gastric stasis.
Oral:
Gastroesophageal reflux disease (GERD), refractory: Short-term (4 to 12 weeks) treatment in adults with documented symptomatic GERD who fail to respond to conventional therapy.
Note: May use metoclopramide as an adjunctive therapy only if gastroparesis is confirmed. The American College of Gastroenterology (ACG) guidelines for the treatment of GERD recommend that diagnostic evaluation to confirm underlying gastroparesis be performed prior to considering the use of prokinetic agents (ACG [Katz 2013]). Furthermore, American Gastroenterological Association (AGA) guidelines for the treatment of GERD recommend against the use of metoclopramide as monotherapy or adjunctive therapy in patients with GERD (AGA [Kahrilas 2008]).
Gastroparesis, diabetic: Relief of symptoms associated with acute and recurrent diabetic gastroparesis in adults.
Off Label Uses
Aspiration prophylaxis in patients undergoing anesthesia
Data from multiple studies of varying methodologies (including randomized, double-blind, placebo-controlled trials) support the use of metoclopramide for the prevention of aspiration in patients undergoing anesthesia, for the treatment of acute tension-type headaches in the emergency department setting.
Metoclopramide description
Each ampoule of injection contains anhydrous metoclopramide HCl (as metoclopramide HCl) 10 mg in 2 mL and sodium chloride in water for injections. When necessary, pH is adjusted with sodium hydroxide and/or hydrochloric acid.
Metoclopramide HCl is 4-amino-5-chloro-N-(2-diethylaminoethyl)-2-methoxybenzamide HCl monohydrate. It has a molecular weight of 354.3 and its molecular formula is C14H22ClN3O2·HCl·H2O.
Metoclopramide hydrochloride occurs as a white or almost white, crystalline powder or crystals, very soluble in water, freely soluble in alcohol, sparingly soluble in methylene chloride, practically insoluble in ether.
Metoclopramide dosage
Therapy with Metoclopramide™ (Metoclopramide) should not exceed 12 weeks in duration.
Instructions for Use/Handling Metoclopramide™ (Metoclopramide)
Just prior to administration, remove the Metoclopramide™ (Metoclopramide) orally disintegrating tablet from the packaging with dry hands. The tablet should be removed from the package and immediately placed on the tongue, to disintegrate and be swallowed with the saliva. The tablet typically disintegrates in about one and one-half minutes. Administration with liquid is not necessary.
Symptomatic Gastroesophageal Reflux Disease
For the relief of symptomatic, documented gastroesophageal reflux disease (GERD), therapy should not exceed 12 weeks.
Administer from 10 mg to 15 mg of Metoclopramide™ (Metoclopramide) orally up to four times daily, 30 minutes before each meal and at bedtime, depending upon symptoms being treated and clinical response. If symptoms occur only intermittently or at specific times of the day, use of metoclopramide in single doses up to 20 mg prior to the provoking situation may be preferred rather than continuous treatment. Occasionally, patients (such as elderly patients) who are more sensitive to the therapeutic or adverse effects of metoclopramide will require only 5 mg per dose.
Experience with esophageal erosions and ulcerations is limited, but healing has thus far been documented in one controlled trial using four times daily therapy at 15 mg/dose, and this regimen should be used when lesions are present, so long as it is tolerated. Because of the poor correlation between symptoms and endoscopic appearance of the esophagus, therapy directed at esophageal lesions is best guided by endoscopic evaluation.
Prolonged treatment ( > 12 weeks) with metoclopramide should be avoided in all but rare cases where therapeutic benefit is thought to counterbalance the risks to the patient of developing tardive dyskinesia..
Diabetic Gastroparesis (Diabetic Gastric Stasis)
For the relief of symptoms associated with diabetic gastroparesis (diabetic gastric stasis), therapy of two to eight weeks is recommended. Therapy should not exceed 12 weeks in duration.
Administer 10 mg of Metoclopramide™ (Metoclopramide) 30 minutes before each meal and at bedtime for two to eight weeks, depending upon response and the likelihood of continued well-being upon drug discontinuation.
The initial route of administration should be determined by the severity of the presenting symptoms. If only the earliest manifestations of diabetic gastric stasis are present, oral administration of Metoclopramide™ (Metoclopramide) may be initiated. However, if severe symptoms are present, therapy should begin with metoclopramide injection (consult labeling of the injection prior to initiating parenteral administration).
Administration of metoclopramide injection up to 10 days may be required before symptoms subside, at which time oral administration may be instituted. Since diabetic gastric stasis is frequently recurrent, Metoclopramide™ (Metoclopramide) therapy should be reinstituted at the earliest manifestation.
Patients with Renal Impairment
Since metoclopramide is excreted principally through the kidneys, in those patients whose creatinine clearance is below 40 mL/min, therapy should be initiated at approximately one-half the recommended dosage. Depending upon clinical efficacy and safety considerations, the dosage may be increased or decreased as appropriate.
How supplied
Dosage Forms And Strengths
Metoclopramide™ (metoclopramide) orally disintegrating tablets contains either 5 mg or 10 mg of metoclopramide base (as monohydrochloride monohydrate). The tablets are white, round, flat-faced, and orange flavored.
Metoclopramide™ (metoclopramide) orally disintegrating tablets 5 mg base (as the monohydrochloride monohydrate) are white, round, flat-faced, orange-flavored and engraved "AP" on one side and "152" on the other side. They are supplied as follows:
Bottles of 100..................NDC 68220-152-10
Metoclopramide™ (metoclopramide) orally disintegrating tablets 10 mg base (as the monohydrochloride monohydrate) are white, round, flat-faced, orange-flavored and engraved "AP"on one side and "153" on the other side. They are supplied as follows:
Bottles of 100..................NDC 68220-153-10
Storage and Handling
Store at 20° to 25°C (68° to 77°F); excursions permitted between 15° to 30°C (59° to 86°F). Protect from moisture.
Dispense in a tight, light-resistant container as defined in the USP/NF.
Manufactured for: Alaven Pharmaceuticals LLC., Marietta, GA 30062. www.alavenpharm.com. For Medical Inquiries, call toll-free 1-888-317-0001. Manufactured by: CIMA® LABS INC.
Metoclopramide interactions
See also:
What other drugs will affect Metoclopramide?
Anticholinergic drugs and narcotic analgesics may antagonise the effects of metoclopramide on gastrointestinal motility.
Alcohol, sedatives, hypnotics, narcotics and tranquilisers have additive sedative effects when administered in conjunction with metoclopramide.
Metoclopramide may cause extrapyramidal symptoms in some patients. Therefore, when metoclopramide is used concomitantly with other drugs that are likely to cause extrapyramidal reactions [eg, neuroleptics (eg, phenothiazines)], caution should be exercised.
Due to its effects on gastric motility, metoclopramide may affect the rate of absorption of drugs from the gastrointestinal tract. Absorption of drugs eg, paracetamol, aspirin in patients with migraine, cyclosporin, diazepam, dopamine, levodopa and morphine-controlled release tablets which are mainly absorbed from the small bowel, may be accelerated. Absorption of drugs eg, digoxin, bromocriptine, cimetidine, penicillin and quinidine which are mainly absorbed from the stomach, may be decreased.
The decrease in gastric emptying time caused by metoclopramide may increase the bioavailability of cyclosporin. Monitoring of cyclosporin concentrations may be necessary.
When metoclopramide is given concurrently with suxamethonium, the recovery time is prolonged.
Since metoclopramide influences the delivery of food to the intestine and thus, the rate of its absorption, the administration of metoclopramide may result in poor diabetic control in some patients. Therefore, adjustment in or timing of insulin dosage may be necessary in insulin-controlled diabetics.
The finding that metoclopramide releases catecholamines in patients with essential hypertension suggests that it should be used cautiously, if at all, in patients receiving monoamine oxidase inhibitors.
Effect on Laboratory Tests: Metoclopramide may blunt the response to the gonadorelin diagnostic test, by increasing serum prolactin levels. It may alter hepatic function test results.
Metoclopramide side effects
See also:
What are the possible side effects of Metoclopramide?
Neurological: Adverse reactions to metoclopramide that are most frequently seen are restlessness, drowsiness, fatigue and lassitude, which occur in approximately 10% of patients. Insomnia, headache, dizziness have been reported less frequently. Acute depression has been reported rarely (<1 in 1000 cases). Symptoms of metoclopramide induced depression have ranged from mild to severe and have included suicidal ideation and suicide. Anxiety or agitation may occur, especially after rapid injection. Delirium, severe dysphoria, obsessive rumination and mania have been reported occasionally.
Parkinsonian symptoms including tremor, rigidity, bradykinesia and akinesia, occur rarely in patients receiving metoclopramide but may be associated with usual or excessive doses or with decreased renal function.
Various extrapyramidal reactions to metoclopramide, usually of the dystonic type, have been reported. Acute dystonic reactions occur in approximately 0.2% of patients treated with metoclopramide 30-40 mg/day. In cancer chemotherapy, patients receiving 1-2 mg/kg/dose, the incidence is 2% in patients over the ages of 30-35, and 25% or higher in children and young adults who have not had prophylactic administration of diphenhydramine. Reactions include spasm of the facial muscles, trismus, rhythmic protrusion of the tongue, a bulbar type of speech, spasm of the extraocular muscles including oculogyric crisis, unnatural positioning of the head and shoulders and opisthotonos. There may be a generalised increase in muscle tone. The majority of reactions occur within 36 hrs of starting treatment and the effects usually disappear within 24 hrs of withdrawal of the drug. However, close observation is required, and in cases of more severe reactions, an antiparkinson drug eg, benztropine or an anticholinergic antihistamine eg, diphenhydramine should be given.
A fatal acute dystonic reaction has been reported in a patient who received hexamethylmelamine, cisplatin and metoclopramide high dose. Dystonic reactions may present rarely as upper airway obstruction with stridor and dyspnoea, possibly secondary to laryngospasm or supraglottic dystonia. A fatal cardiorespiratory arrest occurred in at least 1 patient with an acute dystonic reaction.
Tardive dyskinesia, which may be persistent, has been reported particularly in elderly patients (particularly women) following long-term therapy with metoclopramide. Tardive dyskinesia is most frequently characterised by involuntary movements of the tongue, face, mouth or jaw, and sometimes by involuntary movements of the trunk and/or extremities. The risk of developing tardive dyskinesia and the likelihood that it will become irreversible are believed to increase with increasing duration of therapy and total cumulative dose. Although tardive dyskinesia can occur after relatively brief therapy with the drug at low doses, it appears to be more readily reversible under such circumstances.
Neuroleptic Malignant Syndrome (NMS): It has been reported very rarely (<2 in 10,000). NMS is potentially fatal and comprises hyperpyrexia, altered consciousness, muscle rigidity, autonomic instability and elevated levels of CPK, and must be treated urgently (recognised treatments include dantrolene and bromocriptine).
Metoclopramide should be stopped immediately if NMS occurs.
Gastrointestinal: Nausea or bowel disturbances have been reported.
Cardiovascular: A single case of supraventricular tachycardia following IM administration has been reported. Cardiac conduction abnormalities (eg, bradycardia and heart block) have occurred very rarely (<1 in 10,000) in association with IV metoclopramide. Atrial fibrillation, oedema, ventricular fibrillation, ventricular tachycardia, palpitations and tachycardia have also been associated with the use of metoclopramide. In 1 study in hypertensive patients, IV administered metoclopramide was shown to release catecholamines; hence, caution should be exercised when metoclopramide is used in patients with hypertension.
Endocrine: Raised serum prolactin levels have been observed during metoclopramide therapy; this effect is similar to that noted with many other compounds. Galactorrhoea and breast enlargement have also been observed during metoclopramide therapy.
Hypersensitivity: There have been isolated reports of hypersensitivity reactions (eg, urticaria, maculopapular rash) in patients receiving the drug.
Respiratory: Respiratory failure, secondary to dystonic reaction, acute asthmatic symptoms of wheezing and dyspnoea may occur.
Genitourinary: Urinary incontinence, sexual dysfunction, priapism and muscle spasm may also occur.
Other Effects: There have been isolated reports of blood disorders. Methaemoglobinaemia, particularly following overdose in neonates, has also occurred in patients receiving the drug. Agranulocytosis and hyperthermia have also been observed.
Metoclopramide contraindications
See also:
What is the most important information I should know about Metoclopramide?
NEVER TAKE METOCLOPRAMIDE IN LARGER AMOUNTS THAN RECOMMENDED, OR FOR LONGER THAN 12 WEEKS. High doses or long-term use of metoclopramide can cause a serious movement disorder that may not be reversible. Symptoms of this disorder include uncontrollable muscle movements of your lips, tongue, eyes, face, arms, or legs. The longer you take metoclopramide, the more likely you are to develop a serious movement disorder. The risk of this side effect is higher in women, diabetics, and older adults.
You should not take this medication if you are allergic to metoclopramide, or if you have bleeding or blockage in your stomach or intestines, epilepsy or other seizure disorder, or an adrenal gland tumor (pheochromocytoma).
Before you take metoclopramide, tell your doctor if you have kidney or liver disease, congestive heart failure, high blood pressure, diabetes, Parkinson's disease, or a history of depression.
Do not drink alcohol. It can increase some of the side effects of metoclopramide.
There are many other medicines that can interact with metoclopramide. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor. Keep a list of all your medicines and show it to any healthcare provider who treats you.
Stop using metoclopramide and call your doctor at once if you have tremors or uncontrolled muscle movements, fever, stiff muscles, confusion, sweating, fast or uneven heartbeats, rapid breathing, depressed mood, thoughts of suicide or hurting yourself, hallucinations, anxiety, agitation, seizure, or jaundice (yellowing of your skin or eyes).
Active ingredient matches for Caffeine/Chlorphenamine/Ergotamine/Metamizole/Metoclopramide:
Caffeine/Chlorphenamine/Ergotamine/Metamizole/Metoclopramide
References
- DailyMed. "CAFFEINE; ERGOTAMINE TARTRATE: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
- PubChem. "ERGOTAMINE". https://pubchem.ncbi.nlm.nih.gov/com... (accessed September 17, 2018).
- PubChem. "metoclopramide". https://pubchem.ncbi.nlm.nih.gov/com... (accessed September 17, 2018).
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Information checked by Dr. Sachin Kumar, MD Pharmacology
