Patient leaflets and SmPCs, drug interaction checker, official dosages and NHS pharmacy opening hours — all in one place.
Patient leaflets and SmPCs, drug interaction checker, official dosages and NHS pharmacy opening hours — all in one place.
The electronic medicines compendium (emc) no longer publishes a Summary of Product Characteristics for this product, which usually means it is no longer marketed in the UK. The patient leaflet below is kept for reference, but the product may not be available.
If you were prescribed this medicine, other products containing Amiodarone hydrochloride may still be available. Do not stop your treatment — ask your pharmacist or GP what to use instead.
for 2. What you need to know before you are given Amiodarone Hydrochloride 50 mg/ml
AMIODARONE HYDROCHLORIDE 50 MG/ML Do not use Amiodarone Hydrochloride 50 mg/ml:
Not recommended It is not recommended to use the following medicines at the same time as Amiodarone:
3.
HOW AMIODARONE HYDROCHLORIDE 50 MG/ML IS GIVEN
Amiodarone is given into a vein (intravenously as an injection or infusion) and administered by a doctor or nurse. Dosage The daily dose of Amiodarone Hydrochloride 50 mg/ml depends on the severity of your illness. The dose and the treatment times will be determined by your doctor, who will adjust these especially for you. Unless otherwise prescribed by your doctor, the usual dose is 5 mg per kg of body weight. Your medicine will be injected over a period of at least 3 minutes. When Amiodarone Hydrochloride 50 mg/ml is given as an intravenous injection
The following information is intended for healthcare professionals only: PREPARATION GUIDE FOR:
Amiodarone Hydrochloride 50 mg/ml Concentrate for Solution for Injection/Infusion
In the presence of amiodarone the use of administration equipment containing softening agents such as DEHP (di-2-ethylhexyl phthalate) may cause DEHP to leach into the solution. In order to minimise patient exposure to DEHP, diluted amiodarone solutions for infusion should be administered through sets that do not contain DEHP, such as polyolefin (PE, PP) or glass sets. No other agents may be added to amiodarone infusions. This medicine must not be mixed with other medicines except those mentioned below. Do not mix other preparations in the same syringe. Do not inject other preparations in the same line. If treatment with Amiodarone Hydrochloride 50 mg/ml should be continued, this should be via intravenous infusion.
Adults The usual dose is 5 mg for every kilogram of your weight given over a period of 20 minutes to 2 hours. You may be given another dose of 10 to 20 mg for every kilogram of weight every 24 hours depending on your illness. In an emergency, your doctor may decide to give you a dose of 150 mg to 300 mg as a slow injection over 3 minutes. Your doctor will monitor your response to Amiodarone Hydrochloride 50 mg/ml and the dose will be adjusted accordingly. Children and adolescents There are only limited data on the efficacy and safety in children. Your doctor will decide on an appropriate dose. Elderly As with all patients it is important that the minimum effective dose is used. Your doctor will carefully calculate how much Amiodarone Hydrochloride 50 mg/ml you should get and monitor your heart rate and thyroid function more closely. Your doctor will change you over to amiodarone tablets as soon as possible. If you have received more Amiodarone Hydrochloride 50 mg/ml than you should As this medicine will be given to you whilst you are in hospital or under the care of your doctor it is unlikely that you will be given too much. If, however, you have received higher doses than those recommended you will be carefully monitored by your doctor and will receive supportive therapy if necessary. You may experience the following effects: feeling sick, being sick, constipation or sweating. You may have an abnormally slow or fast heartbeat. If you have any further question on the use of this medicine, ask your doctor or other healthcare professional.
4.
POSSIBLE SIDE EFFECTS
Like all medicines, this medicine can cause side effects, although not everybody gets them. Amiodarone Hydrochloride 50 mg/ml may stay in your blood for up to a month after stopping treatment. You may still get side effects in this time. Stop having Amiodarone Hydrochloride 50 mg/ml and tell a doctor, nurse or pharmacist or go to a hospital straight away if: Very rare (affects less than 1 in 10,000 people)
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4. Possible side effects 5. How to store Amiodarone Hydrochloride 50 mg/ml 6. Contents of the pack and other information
1.
WHAT AMIODARONE HYDROCHLORIDE 50 MG/ML IS AND WHAT IT IS USED FOR
Amiodarone is used to treat irregular beating of your heart called "arrhythmias". Amiodarone works by controlling your heart if it is not beating normally. Amiodarone Hydrochloride 50 mg/ml is given when a quick response is needed or if you are unable to take tablets. Your doctor will give you this medicine and you will be monitored under hospital or specialist supervision.
2.
not listed in this leaflet. You can also report side effects directly via the Yellow Card Scheme, Website: www.mhra.gov.uk/yellowcard or search for MHRA Yellow Card in the Google Play or Apple App Store. By reporting side effects you can help provide more information on the safety of this medicine.
5.
AMIODARONE HYDROCHLORIDE 50 MG/ML
6.
What Amiodarone Hydrochloride 50 mg/ml contains The active substance is amiodarone hydrochloride. Each millilitre concentrate for solution for injection/infusion contains 50 milligrams (mg) of amiodarone hydrochloride equivalent to 46.9 mg amiodarone. 1 ampoule with 3 ml Amiodarone Hydrochloride 50 mg/ml contains 150 mg amiodarone hydrochloride. One ampoule of Amiodarone Hydrochloride 50 mg/ml diluted as recommended in 250 ml of glucose 5% results in a concentration of 0.6 mg/ml of amiodarone hydrochloride. The other ingredients are polysorbate 80 (E433), benzyl alcohol and water for injections. What Amiodarone Hydrochloride 50 mg/ml looks like and contents of the pack Clear, pale yellow sterile solution. Pack sizes: Amiodarone Hydrochloride 50 mg/ml is available as 5 ml glass ampoule with 3 ml concentrate for solution for injection/ infusion in packs of 5 or 10. Marketing Authorisation Manufacturer
Holder
and
Marketing Authorisation Holder: hameln pharma ltd Nexus, Gloucester Business Park Gloucester, GL3 4AG, United Kingdom Manufacturer: HBM Pharma s.r.o. Sklabinská 30 03680 Martin Slovak Republic hameln rds s.r.o. Horná 36 90001 Modra Slovak Republic This medicinal product is authorised in the Member States of the EEA under the following names:
AT
Amiodaron-hameln 50 mg/ml Konzentrat zur Herstellung einer Injektions- /Infusionslösung
BG Amiodaron hameln 50 mg/ml CZ DE
Amiodaron hameln Amiodaron-hameln 50 mg/ml Konzentrat zur Herstellung einer Injektions-/Infusionslösung
DK FI
Amiodaron hameln Amiodaron hameln 50 mg/ml injektio/ infuusiokonsentraatti, liuosta varten
HR
Amiodaronklorid hameln 50 mg/ml koncentrat za otopinu za injekciju/ infuziju
HU Amiodaron hameln 50 mg/ml NL
Amiodaron HCl hameln 50 mg/ml
NO Amiodaron hameln PL
Amiodaron hameln
RO Amiodaronă hameln 50 mg/ml concentrat pentru soluție injectabilă / perfuzabilă SE
Amiodaron hameln
SI
Amjodaron hameln 50 mg/ml koncentrat za raztopino za injiciranje/ infundiranje
SK UK
Amiodaron hameln 50 mg/ml Amiodarone Hydrochloride 50 mg/ml Concentrate for Solution for Injection/ Infusion
This leaflet was last revised in 07/2022. 1036/26/22
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Before use, the sterile concentrate should be visually inspected for clarity, particulate matter, discolouration and the integrity of the container. The solution should only be used if it is clear and the container is undamaged and intact. Dilution
The medicine should be diluted with glucose 5%. For each ampoule, a maximum of 250 ml glucose 5% should be used. Greater dilutions are unstable. Amiodarone, diluted in a glucose 5% solution to a concentration of < 0.6 mg/ml, is not stable. Solutions containing less than 2 Amiodarone Hydrochloride 50 mg/ml ampoules in 500 ml of glucose 5% are unstable and must not be used. The dilution is to be made under aseptic conditions. The solution is to be inspected visually for particulate matter and discoloration prior to administration. The solution should only
be used if the solution is clear and free from particles. Stability in solution The diluted product is physically and chemically stable for 24 hours at 25°C. However, from a microbiological viewpoint, the medicine should be used immediately after dilution. If not used immediately, in-use storage times and conditions prior to use are the responsibility of the user and would normally not be longer than 24 hours at 2 to 8°C, unless dilution has taken place in controlled and validated aseptic conditions. Storage Do not store above 25°C. Do not refrigerate or freeze. Keep the ampoules in the outer carton in order to protect from light. For single dose use only. Any unused medicine or waste material should be disposed of in accordance with local requirements.
Amiodarone Hydrochloride 50 mg/ml Concentrate for Solution for Injection/Infusion comes as injection containing 50mg/ml. Always follow the dose your doctor or pharmacist has given you, and read the leaflet that comes with the medicine.
The active substance in Amiodarone Hydrochloride 50 mg/ml Concentrate for Solution for Injection/Infusion is amiodarone hydrochloride.
This leaflet reproduces the patient information leaflet approved for Amiodarone Hydrochloride 50 mg/ml Concentrate for Solution for Injection/Infusion, as published on the electronic medicines compendium (emc). The version printed inside your medicine’s packaging is the one that applies to you.
Whether a medicine is available over the counter or on prescription only depends on its licence. Check the leaflet, or ask your pharmacist — they can tell you straight away.
The text above reproduces the patient information leaflet approved for this medicine, restructured for easier reading.
Amiodarone hydrochloride is indicated for the treatment of serious cardiac arrhythmias, in cases where other therapies are not effective or contraindicated:
- atrial arrhythmias, including atrial fibrillation or flutter
- AV nodal arrhythmias and AV reentrant tachycardia, e.g. as a manifestation of Wolff-Parkinson-White syndrome
- life-threatening ventricular arrhythmias, including persistent or non-persistent ventricular tachycardia or episodes of ventricular fibrillation
Amiodarone Hydrochloride 50 mg/ml Concentrate for Solution for Injection/Infusion can be used where a rapid response is required or where oral administration is not possible.
Amiodarone hydrochloride may be used prior to DC cardioversion.
Treatment should be initiated and normally monitored only under hospital or specialist supervision.
Amiodarone hydrochloride should only be used when facilities exist for cardiac monitoring, defibrillation, and cardiac pacing.
Thyroid function test should be performed where appropriate prior to therapy in all patients.
Posology
The standard recommended dose is 5mg/kg bodyweight given by intravenous infusion over a period of 20 minutes to 2 hours. This should be administered as a dilute solution in 250ml glucose 5%. This may be followed by repeat infusion up to 1200mg (approximately 15mg/kg bodyweight) in up to 500ml glucose 5% per 24 hours, the rate of infusion being adjusted on the basis of clinical response (see section 4.4).
In extreme clinical emergency the drug may, at the discretion of the clinician, be given as a slow intravenous injection of 150-300mg in 10-20ml glucose 5% over a minimum of 3 minutes. This should not be repeated for at least 15 minutes. Patients treated in this way with amiodarone hydrochloride must be closely monitored, e.g. in an intensive care unit (see section 4.4).
Changeover from intravenous to oral therapy
As soon as an adequate response has been obtained, oral therapy should be initiated concomitantly at the usual loading dose (i.e. 200mg three times a day). Amiodarone hydrochloride should then be phased out gradually.
Paediatric population
The safety and efficacy of amiodarone in children and adolescents has not been established. Currently available data are described in sections 5.1 and 5.2. Due to the presence of benzyl alcohol, intravenous Amiodarone Hydrochloride 50 mg/ml Concentrate for Solution for Injection/Infusion is contraindicated in neonates (see section 4.3) and should be used with caution in infants and children up to 3 years old (see section 4.4).
Elderly
As with all patients it is important that the minimum effective dose is used. Whilst there is no evidence that dosage requirements are different for this group of patients they may be more susceptible to bradycardia and conduction defects if too high a dose is employed. Particular attention should be paid to monitoring thyroid function (see sections 4.3, 4.4 and 4.8).
Cardiopulmonary resuscitation
The recommended dose for ventricular fibrillations/pulseless ventricular tachycardia resistant to defibrillation is 300 mg (or 5 mg/kg body-weight) diluted in 20 ml glucose 5% and rapidly injected. An additional 150 mg (or 2.5 mg/kg body-weight) IV dose may be considered if ventricular fibrillation persists.
See section 6.2 for information on incompatibilities.
Hepatic and renal impairment
Although no dosage adjustment for patients with renal or hepatic abnormalities has been defined during chronic treatment with oral amiodarone, close clinical monitoring is prudent for elderly patients e.g. in an intensive care unit.
Method of administration
Intravenous use.
Via infusion: For instructions on dilution of the medicinal product before administration, see section 6.6.
- Hypersensitivity to the active substance, iodine or to any of the excipients listed in section 6.1. (One ampoule contains approximately 56 mg iodine.)
- Due to the presence of benzyl alcohol, intravenous Amiodarone Hydrochloride 50 mg/ml Concentrate for Solution for Injection/Infusion is contraindicated in neonates.
- Severe respiratory failure, circulatory collapse, or severe arterial hypotension; hypotension, heart failure and cardiomyopathy are also contraindications when using Amiodarone Hydrochloride 50 mg/ml as a bolus injection.
- Evidence or history of thyroid dysfunction (see section 4.2 and 4.4).
- Sinus bradycardia, sino-atrial heart block and sick sinus syndrome in patients without a pacemaker. In patients with severe conduction disturbances (high grade AV block, bifascicular or trifascicular block) or sinus node disease, amiodarone should be used only in specialized units in conjunction with a pacemaker.
- Concomitant use of medicinal products which prolong the QT interval (see section 4.5).
- Pregnancy and lactation. The use is allowed only in special life-threatening circumstances as specified in sections 4.1, 4.4 and 4.6.
The above contraindications do not apply to the use of amiodarone hydrochloride for cardiopulmonary resuscitation of shock-resistant ventricular fibrillation.
Contains benzyl alcohol (22.2 mg/ml).
Benzyl alcohol may cause toxic and allergic reactions. The minimum amount of benzyl alcohol at which toxicity may occur is not known with an increased risk in young children due to accumulation.
The administration of medications containing benzyl alcohol to newborns or premature neonates has been associated with serious adverse events and a fatal “Gasping Syndrome” (symptoms include a striking onset of gasping syndrome, hypotension, bradycardia and cardio-vascular collapse). This medicinal product is contraindicated in neonates (see section 4.3) and should be used with caution in infants and young children up to 3 years old (see section 4.2).
As benzyl alcohol may cross the placenta, this medicinal product should be used with caution in pregnancy (see section 4.3 and 4.6).
High volumes of medications containing benzyl alcohol should be used with caution and only if necessary, especially in subjects with liver or kidney impairment because of the risk of accumulation and toxicity (metabolic acidosis).
Administration:
Amiodarone hydrochloride should only be used in a special care unit under continuous monitoring (ECG and blood pressure).
Intravenous infusion is preferred to intravenous bolus due to the haemodynamic effects sometimes associated with rapid injection (see section 4.8). Circulatory collapse may be precipitated by too rapid administration or overdosage (atropine has been used successfully in such patients presenting with bradycardia). Repeated or continuous infusion via peripheral veins may lead to injection site reactions (see section 4.8). When repeated or continuous infusion is anticipated, administration by a central venous catheter is recommended.
Amiodarone should not be mixed with other preparations in the same syringe and should not be injected with other preparations in the same line. If treatment with amiodarone should be continued, this should be via intravenous infusion (see section 4.2).
When given by infusion amiodarone hydrochloride may reduce drop size and, if appropriate, adjustments should be made to the rate of infusion.
Anaesthesia (see section 4.5): Before surgery, the anaesthetist should be informed that the patient is taking amiodarone.
Reports of crystallisation have been received for hameln Amiodarone Hydrochloride 50 mg/ml Concentrate for Solution for Injection/Infusion:
• Inspect each ampoule and check for crystalline content prior to administration. The solution should only be used if it is clear, free from particles and the container is undamaged and intact.
• Consider the use of in-line filters as an additional precautionary measure.
Cardiac disorders:
Caution should be exercised in patients with hypotension and decompensated cardiomyopathy and severe heart failure (also see section 4.3).
Amiodarone has a low pro-arrhythmic effect. Onsets of new arrhythmias or worsening of treated arrhythmias, sometimes fatal, have been reported. It is important, but difficult to differentiate a lack of efficacy of the drug from a proarrhythmic effect, whether or not this is associated with a worsening of the cardiac condition. Proarrhythmic effects generally occur in the context of QT prolongation factors such as drug interactions and/or electrolytic disorders (see sections 4.5 and 4.8). Despite QT interval prolongation, amiodarone exhibits a low torsadogenic activity.
Too high a dosage may lead to severe bradycardia and to conduction disturbances with the appearance of an idioventricular rhythm, particularly in elderly patients or during cardiac glycoside therapy. In these circumstances, amiodarone hydrochloride treatment should be withdrawn. If necessary beta-adrenostimulants or glucagon may be given. Because of the long half-life of amiodarone, if bradycardia is severe and symptomatic the insertion of a pacemaker should be considered.
The pharmacological action of amiodarone induces ECG changes: QT prolongation (related to prolonged repolarisation) with the possible development of U-waves and deformed T-waves; these changes do not reflect toxicity.
Severe bradycardia and heart block after sofosbuvir
Life-threatening cases of bradycardia and heart block have been observed when sofosbuvir-containing regimens are used in combination with amiodarone.
Bradycardia has generally occurred within hours to days, but later cases have been mostly observed up to 2 weeks after initiating HCV treatment.
Amiodarone should only be used in patients on sofosbuvir-containing regimen when other alternative anti-arrhythmic treatments are not tolerated or are contraindicated.
Should concomitant use of amiodarone be considered necessary, it is recommended that patients undergo cardiac monitoring in an in-patient setting for the first 48 hours of coadministration, after which outpatient or self-monitoring of the heart rate should occur on a daily basis through at least the first 2 weeks of treatment.
Due to the long half-life of amiodarone, cardiac monitoring as outlined above should also be carried out for patients who have discontinued amiodarone within the past few months and are to be initiated on sofosbuvir- containing regimen.
All patients receiving amiodarone in combination with sofosbuvir-containing regimen should be warned of the symptoms of bradycardia and heart block and should be advised to seek medical advice urgently should they experience them.
Primary graft dysfunction (PGD) post cardiac transplant:
In retrospective studies, amiodarone use in the transplant recipient prior to heart transplant has been associated with an increased risk of PGD.
PGD is a life-threatening complication of heart transplantation that presents as a left, right or biventricular dysfunction occurring within the first 24 hours of transplant surgery for which there is no identifiable secondary cause (see section 4.8). Severe PGD may be irreversible.
For patients who are on the heart transplant waiting list, consideration should be given to use an alternative antiarrhythmic drug as early as possible before transplant.
General anaesthesia:
Caution is advised in patients undergoing general anaesthesia, or receiving high dose oxygen therapy.
Potentially severe complications have been reported in patients taking amiodarone undergoing general anaesthesia: bradycardia unresponsive to atropine, hypotension, disturbances of conduction, decreased cardiac output (see section 4.5).
Endocrine disorders (see section 4.8):
Amiodarone may induce hyperthyroidism, particularly in patients with a personal history of thyroid disorders or patients who are taking/have previously taken oral amiodarone. Serum ultrasensitive thyroid-stimulating hormone (usTSH) level should be measured when thyroid dysfunction is suspected. Thyroid function tests should be performed where appropriate prior to therapy in all patients.
Amiodarone contains iodine and thus may interfere with radio-iodine uptake. However, thyroid function tests (free-T3, free-T4, usTSH) remain interpretable. Amiodarone inhibits peripheral conversion of thyroxine (T4) to triiodothyronine (T3) and may cause isolated biochemical changes (increase in serum free-T4, free-T3 being slightly decreased or even normal) in clinically euthyroid patients. There is no reason in such cases to discontinue amiodarone treatment if there is no clinical or further biological (usTSH) evidence of thyroid disease.
Respiratory, thoracic and mediastinal disorders (see section 4.8):
Onset of dyspnoea or non-productive cough may be related to pulmonary toxicity such as interstitial pneumonitis. Very rare cases of interstitial pneumonitis have been reported with intravenous amiodarone. When the diagnosis is suspected, a chest X-ray should be performed. Amiodarone therapy should be re-evaluated since interstitial pneumonitis is generally reversible following early withdrawal of amiodarone, and corticosteroid therapy should be considered (see section 4.8). Clinical symptoms often resolve within a few weeks followed by slower radiological and lung function improvement. Some patients can deteriorate despite discontinuing amiodarone hydrochloride. Fatal cases of pulmonary toxicity have been reported.
Very rare cases of severe respiratory complications, sometimes fatal, have been observed usually in the period immediately following surgery (adult acute respiratory distress syndrome); a possible interaction with a high oxygen concentration may be implicated (see sections 4.5 and 4.8).
Hepato-biliary disorders (see section 4.8):
Severe hepatocellular insufficiency may occur within the first 24 hours of IV amiodarone, and may sometimes be fatal. Close monitoring of transaminases is therefore recommended as soon as amiodarone is started.
Severe bullous reactions:
Life-threatening or even fatal cutaneous reactions: Stevens-Johnson syndrome (SJS), Toxic Epidermal Necrolysis (TEN) (see section 4.8). If symptoms or signs of SJS, TEN (e.g. progressive skin rash often with blisters or mucosal lesions) are present, amiodarone treatment should be discontinued immediately.
Eye disorders (see section 4.8):
If blurred or decreased vision occurs, complete ophthalmologic examination including fundoscopy should be promptly performed. Appearance of optic neuropathy and/or optic neuritis requires amiodarone withdrawal due to the potential progression to blindness.
Drug interactions (see section 4.5):
Concomitant use of amiodarone with the following drugs is not recommended; beta-blockers, heart rate lowering calcium channel inhibitors (verapamil, diltiazem), stimulant laxative agents which may cause hypokalaemia.
In cases of hypokalaemia, corrective action should be taken and QT interval monitored. In case of torsade de pointes antiarrhythmic agents should not be given; pacing may be instituted and IV magnesium may be used.
Increased plasma levels of flecainide have been reported with co-administration of amiodarone. The flecainide dose should be reduced accordingly and the patient closely monitored.
Drugs inducing “Torsade de Pointes” or prolonging the QT interval
Some of the more important drugs that interact with amiodarone include warfarin, digoxin, phenytoin and any drug which prolongs the QT interval.
Combined therapy with the following drugs which prolong the QT interval is contra-indicated (see section 4.3) due to the increased risk of torsade de pointes; for example:
• Class Ia anti-arrhythmic drugs e.g. quinidine, procainamide, disopyramide;
• Class III anti-arrhythmic drugs e.g. sotalol, bretylium;
• intravenous erythromycin, co-trimoxazole or pentamidine injection;
• some anti-psychotics e.g. chlorpromazine, thioridazine, fluphenazine, pimozide, haloperidol, amisulpiride and sertindole;
• lithium and tricyclic anti-depressants e.g. doxepin, maprotiline, amitriptyline;
• certain antihistamines e.g. terfenadine, astemizole, mizolastine;
• anti-malarials e.g. quinine, mefloquine, chloroquine, halofantrine;
• moxifloxacin.
Fluoroquinolones
There have been rare reports of QTc interval prolongation, with or without torsade de pointes, in patients taking amiodarone with fluoroquinolones. Concomitant use of amiodarone with fluoroquinolones should be avoided (concomitant use with moxifloxacin is contra-indicated, see above).
Drugs lowering heart rate, causing automaticity or conduction disorders
Combined therapy with the following drugs is not recommended:
• Beta blockers and certain calcium channel inhibitors (diltiazem, verapamil); potentiation of negative chronotropic properties and conduction slowing effects may occur.
• Sofosbuvir: Coadministration of amiodarone with sofosbuvir-containing regimens may lead to serious symptomatic bradycardia. If coadministration cannot be avoided, cardiac monitoring is recommended (see section 4.4).
• Stimulant laxatives, which may cause hypokalaemia thus increasing the risk of “torsade de pointes”; other types of laxatives should be used.
Combined therapy with the following drugs which may also cause hypokalaemia and/or hypomagnesaemia should be considered with caution:
• diuretics,
• systemic corticosteroids,
• tetracosactide,
• intravenous amphotericin B.
General anaesthesia
Potentially severe complications such as bradycardia unresponsive to atropine, hypotension, disturbances of conduction, decreased cardiac output have been reported in patients taking amiodarone undergoing general anesthesia (see section 4.4).
Very rare cases of severe respiratory complications (adult acute respiratory distress syndrome), sometimes fatal, have been observed usually in the period immediately following surgery. A possible interaction with a high oxygen concentration may be implicated (see section 4.4).
Effect of amiodarone hydrochloride on other medicinal products
Amiodarone and/or its metabolite, desethylamiodarone, inhibit CYP1A1, CYP1A2, CYP3A4, CYP2C9, CYP2D6 and P-glycoprotein and may increase exposure of their substrates. Due to the long half-life of amiodarone, interactions may be observed for several months after discontinuation of amiodarone.
PgP Substrates
Amiodarone is a P-gp inhibitor. Co administration with P-gp substrates is expected to result in an increase in their exposure.
Digoxin
Administration of amiodarone hydrochloride to a patient already receiving digoxin will bring about an increase in the plasma digoxin concentration and thus precipitate symptoms and signs associated with high digoxin levels; disturbances in automaticity (excessive bradycardia), a synergistic effect on heart rate and atrioventricular conduction may occur. Clinical, ECG and biological monitoring is recommended to observe for signs of cardiac glycoside toxicity and digoxin dosage should be halved.
Dabigatran
Caution should be exercised when amiodarone is co administered with dabigatran due to the risk of bleeding. It may be necessary to adjust the dosage of dabigatran as per its label.
CYP2C9 substrates
Amiodarone raises the plasma concentrations of CYP 2C9 substrates such as oral anticoagulants (warfarin) and phenytoin by inhibition of the cytochrome P450 2C9.
Warfarin
The dose of warfarin should be reduced accordingly. More frequent monitoring of prothrombin time both during and after amiodarone treatment is recommended.
Phenytoin
Phenytoin dosage should be reduced if signs of overdosage appear, and plasma levels may be measured.
CYP2D6 substrates
Flecainide
Given that flecainide is mainly metabolised by CYP 2D6, by inhibiting this isoenzyme, amiodarone may increase flecainide plasma levels; it is advised to reduce the flecainide dose by 50% and to monitor the patient closely for adverse effects. Monitoring of flecainide plasma levels is strongly recommended in such circumstances.
CYP P450 3A4 substrates
When drugs are co-administered with amiodarone, an inhibitor of CYP 3A4, this may result in a higher level of their plasma concentrations, which may lead to a possible increase in their toxicity:
• Ciclosporin: plasma levels of ciclosporin may increase as much as 2-fold when used in combination. A reduction in the dose of ciclosporin may be necessary to maintain the plasma concentration within the therapeutic range.
• Statins: the risk of muscular toxicity (e.g. rhabdomyolysis) is increased by concomitant administration of amiodarone with statins metabolised by CYP 3A4 such as simvastatin, atorvastatin and lovastatin. It is recommended to use a statin not metabolised by CYP 3A4 when given with amiodarone.
• Other drugs metabolised by cytochrome P450 3A4: examples of such drugs are lidocaine, sirolimus, tacrolimus, sildenafil, fentanyl, midazolam, triazolam, dihydroergotamine, ergotamine and colchicine
Interaction with substrates of other CYP 450 isoenzymes
In vitro studies show that amiodarone also has the potential to inhibit CYP 1A2, CYP 2C19 and CYP 2D6 through its main metabolite. When co-administered, amiodarone would be expected to increase the plasma concentration of drugs whose metabolism is dependent upon CYP 1A2, CYP 2C19 and CYP 2D6.
Effect of other products on amiodarone hydrochloride
CYP3A4 inhibitors and CYP2C8 inhibitors may have a potential to inhibit amiodarone metabolism and to increase its exposure. It is recommended to avoid CYP 3A4 inhibitors (e.g. grapefruit juice and certain medicinal products) during treatment with amiodarone. Grapefruit juice inhibits cytochrome P450 3A4 and may increase the plasma concentration of amiodarone. Grapefruit juice should be avoided during treatment with oral amiodarone.
Pregnancy
Data on a limited number of exposed pregnancies are available. Amiodarone and N-desmethylamiodarone cross the placental barrier and achieve 10-25% of the maternal plasma concentrations in the infant. Most frequent complications include impaired growth, preterm birth and impaired function of the thyroid gland in newborn babies. Hypothyroidism, bradycardia and prolonged QT intervals were observed in approximately 10% of the newborn babies. In isolated cases an increased thyroid gland or cardiac murmurs were found. The malformation rate does not appear to be increased. However, the possibility of cardiac defects should be kept in mind. Therefore, amiodarone must not be used during pregnancy unless clearly necessary and the real risk of reoccurrence of life threatening arrhythmias should be weighed against the possible hazard for the foetus. Given the long half-life of amiodarone, women of child-bearing age would need to plan for a pregnancy starting at least half a year after finishing therapy, in order to avoid exposure of the embryo/foetus during early pregnancy.
Lactation
The passage into mother's milk is proven for the active ingredient and for the active metabolite. If therapy is required during the lactation period, or if amiodarone was taken during pregnancy, breast-feeding should be stopped. The use is allowed only in special life-threatening circumstances as specified in sections 4.1, 4.3 and 4.4.
Fertility
Elevated serum levels of Luteinizing hormone (LH) and Follicle-stimulating hormone (FSH) were found in male patients after long-term treatment indicating testicular dysfunctions.
Amiodarone hydrochloride may affect the ability to drive or use machines.
The most common adverse drug effects reported with intravenous amiodarone hydrochloride are infusion phlebitis, bradycardia, and hypotension.
Table 1: Frequency of the adverse reaction
System Organ Class
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)
Not known
(cannot be estimated from the available data)
Blood and lymphatic system disorders
- In patients taking amiodarone there have been incidental findings of bone marrow granulomas. The clinical significance of this is unknown
- Neutropenia
- Agranulocytosis
Immune system disorders
Anaphylactic shock.
Angioneurotic oedema (Quincke's oedema)
Endocrine disorders
Syndrome of inappropriate antidiuretic hormone secretion (SIADH).
-Hyperthyroidism, sometimes fatal (see section 4.4).
-Hypothyroidism.
Psychiatric disorders
Libido decreased
- Delirium (including confusion).
- Hallucination
Nervous system disorders
Extrapyramidal tremor.
Peripheral sensorimotor neuropathy and/or myopathy, usually reversible on withdrawal of the drug.
- Benign intracranial hypertension (pseudo-tumour cerebri).
- Headache.
Eye disorders
Microdeposits at the anterior surface of the cornea are found in almost every patient, which are usually limited to the area below the pupil. They may be associated with colored halos in dazzling light or blurred vision. They usually regress 6-12 months after discontinuation of amiodarone hydrochloride.
Optic neuropathy/ neuritis that may progress to blindness (see section 4.4).
Cardiac disorders
Dose-dependent bradycardia.
- Severe bradycardia (in cases of sinus node dysfunction and in the elderly) or (more rarely) sinus arrest: this may necessitate discontinuation of the treatment.
- Occurrence of new - and exacerbation of existing - arrhythmias, sometimes followed by cardiac arrest (see also section 4.4 and section 4.5).
- Conduction disturbances (sinoatrial block, AV block).
Torsades de pointes (see section 4.4)
Vascular disorders
Hypotension and increased heart rate immediately following injection. These are generally moderate and transient in nature. Cases of severe hypotension or shock have been reported following overdose or too rapid administration (bolus injection).
Hot Flushes.
Respiratory, thoracic and mediastinal disorders
- Interstitial pneumonitis or fibrosis, sometimes fatal (see section 4.4).
- Acute adult respiratory distress syndrome, sometimes with fatal sequelae.
- Bronchospasm and/or apnoea in patients with serious respiratory problems, especially patients with asthma.
Gastrointestinal disorders
Nausea.
Pancreatitis (acute).
Hepatobiliary disorders
- A mild to moderate increase in transaminase levels (1.5 to 3 times above normal) at the start of treatment, which is often transient in nature and resolves spontaneously upon lowering the dose.
- Acute liver function disorders, with increased serum transaminase and/or jaundice, including hepatic failure, sometimes with fatal sequelae (see section 4.4).
Skin and subcutaneous tissue disorders
Eczema.
Sweating.
- Urticaria.
- Severe skin reaction as toxic epidermal necrolysis (TEN)/Stevens- Johnson syndrome (SJS), bullous dermatitis and Drug reaction with eosinophilia and systematic symptoms (DRESS).
Musculoskeletal and Connective Tissue Disorders
Back pain.
Reproductive system and breast disorders
Libido decreased
General disorders and administration site conditions
At the site of injection or infusion: pain, erythema, oedema, necrosis, extravasation, infiltration, inflammation, induration, thrombophlebitis, phlebitis, cellulitis, infection, pigmentation changes.
The excipient benzyl alcohol may cause hypersensitivity reactions.
Injury, poisoning and procedural complications
Primary graft dysfunction post cardiac transplant (see section 4.4).
A few rare cases with various clinical symptoms, indicative of hypersensitivity reactions, have been reported: vasculitis, reduced renal function with a rise in creatinine levels, thrombocytopenia, anaphylaxis.
Reporting of suspected adverse reactions
Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the Yellow Card Scheme Website: www.mhra.gov.uk/yellowcard or search for MHRA Yellow Card in the Google Play or Apple App Store.
There is no information regarding overdosage with intravenous amiodarone.
In cases of acute overdose or too rapid intravenous administration, the following can be observed: nausea, vomiting, constipation, sweating, bradycardia and prolonged QT interval. Following substantial overdose, onset of hypotension, heart block and Torsades de Pointes should also be expected. In exceptional cases, hyperthyroidism may occur.
Following substantial overdose, prolonged ECG monitoring must be performed. Intensive care unit admission should be considered. Hypotension can be treated with infusion fluids or vasopressors. The use of alpha- or beta adrenergic agents or temporary pacing may be indicated. Class Ia and III antiarrhythmic agents should be avoided, as they are associated with QT interval prolongation and induction of Torsades de Pointes. Further treatment should be supportive and symptomatic.
Amiodarone and its metabolites cannot be dialysed.
Due to the pharmacokinetics of amiodarone, adequate and prolonged surveillance of the patient, particularly cardiac status, is recommended.
Medicines sold in Romania with the same active substance: Cunoscut în România ca
Same active substance. The strength, the form and whether you need a prescription can differ. Always ask a pharmacist before you switch. Romanian medicines in the UK →
Medicines sold in Poland with the same active substance: W Polsce znany jako
Same active substance. The strength, the form and whether you need a prescription can differ. Always ask a pharmacist before you switch. Polish medicines in the UK →
Ask anything about Amiodarone Hydrochloride 50 mg/ml Concentrate for Solution for Injection/Infusion. The assistant answers only from this leaflet — if the leaflet does not cover it, it will say so. It does not give medical advice.
Answers come from the patient leaflet published on the electronic medicines compendium (emc). They are not medical advice. Ask a pharmacist or your GP if you are unsure. For urgent help call NHS 111, or 999 in an emergency.
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