Drugs List

Therapeutic Indications

Uses

Treatment of manic episodes associated with bipolar disorder

Treatment of moderate to severe manic episodes associated with bipolar I disorder in adults.

Contraindications

Children under 18 years
Breastfeeding
Renal impairment - creatinine clearance below 15ml/minute
Severe hepatic impairment

Precautions and Warnings

Family history of long QT syndrome
Patients over 65 years
Predisposition to hypotension
Cardiovascular disorder
Cerebrovascular disorder
Dementia
Diabetes mellitus
Epileptic disorder
History of seizures
Moderate hepatic impairment
Parkinson's disease
Pregnancy

Patients at risk of suicide should be closely supervised
Advise ability to drive/operate machinery may be affected by side effects
Advise patients not eat immediately after a dose
Monitor ECG in patients at risk of QT prolongation
Monitor patients with existing or tendency towards diabetes mellitus
Neonate exposed in utero: Monitor neonate for adverse effects
Advise patient to report unexplained fever, sore throat, bruising, bleeding
Consider discontinuation if signs of tardive dyskinesia occur
Dysphagia & aspiration:caution in patients at risk for aspiration pneumonia
May cause postural hypotension especially in elderly
May impair ability to reduce core body temperature
Discontinue if patient develops neuroleptic malignant syndrome
Advise patient to avoid alcohol during treatment

Elderly patients with psychosis related to dementia, treated with antipsychotic substances, are at an increased risk of death.

Patients with Parkinson's disease or dementia with Lewy Bodies are at increased risk of Neuroleptic Malignant Syndrome and increased sensitivity to antipsychotics.

Pregnancy and Lactation

Pregnancy

Use asenapine with caution in pregnancy.

Use of asenapine during pregnancy is recommended by the manufacturer only if the benefits to the mother outweigh the potential risk to the foetus. There are no adequate data from the use of asenapine in pregnant women.

In animal studies asenapine did not impair fertility in rats and was not found to be teratogenic in rats and rabbits. Embryotoxic effects were, however, found in reproduction toxicology studies using rats and rabbits and asenapine caused mild maternal toxicity and slight retardation of foetal skeletal development.

Neonates exposed to antipsychotics during the third trimester of pregnancy are at risk of adverse reactions. Monitor neonates carefully for extrapyramidal and/or withdrawal symptoms.

The use of all medication in pregnancy should be avoided whenever possible; particularly in the first trimester. Non-drug treatments should also be considered. When essential, a medication with the best safety record over time should be chosen, employing the lowest effective dose for the shortest possible time. Polypharmacy should be avoided. Teratogens taken in the pre-embryonic period, often quoted as lasting until 14-17 days post-conception, are believed to have an all-or-nothing effect. Where drugs have a short half-life, and when the date of conception is certain, this may allow women to be reassured where drug exposure has occurred within this time frame. Further advice may be available from the UK National Teratology Information Service (NTIS) and through ToxBase, available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).

Lactation

Asenapine is contraindicated while breastfeeding.

Studies in rats have shown asenapine to be excreted in milk during lactation. It is not known if asenapine or its metabolites are excreted in human milk.

Neonates, infants born prematurely, those with low birth weight, those with an unstable gastrointestinal function or who have serious illnesses may require special consideration. For any infant, if a drug is prescribed to the nursing mother, it should be at the lowest practical dose and for the shortest time. When drug administration is unavoidable and breastfeeding is to continue, minimisation of exposure of the infant to the drug may sometimes be achieved by timing the maternal doses to just after a feeding episode. Infants exposed to drugs via breast milk should be monitored for unusual signs or symptoms. Interactions between the drug received by the infant from the mother's milk and medication prescribed for the infant should also be considered, for example, when the drug given to the infant may prevent metabolism of the drug received via breast milk.
Specialist advice is available from the UK Drugs in Lactation Advisory Service at https://www.midlandsmedicines.nhs.uk/content.asp?section=6&subsection=17&pageIdx=1

Side Effects

Akathisia
Allergic reaction
Amenorrhoea
Anaphylactic reaction
Angioedema
Anxiety
Bundle branch block
Dizziness
Dysarthria
Dysgeusia
Dyskinesia
Dysphagia
Dystonia
Exacerbation of diabetes
Extrapyramidal effects
Fatigue
Galactorrhoea
Glossodynia
Gynaecomastia
Hyperglycaemia
Hyperprolactinaemia
Hypersalivation
Hypersensitivity reactions
Hypotension
Increased appetite
Increases in hepatic enzymes
Mouth inflammation
Muscle rigidity
Nausea
Neuroleptic malignant syndrome
Neutropenia
Oral hypoaesthesia
Oral mucosal blistering
Oral paraesthesia
Oral ulceration
Orthostatic hypotension
Parkinsonism
Prolongation of QT interval
Pulmonary embolism
Restless legs
Rhabdomyolysis
Sedation
Seizures
Sexual dysfunction
Sinus bradycardia
Sinus tachycardia
Somnolence
Syncope
Throat swelling
Tongue swelling
Visual disturbances
Weight gain

Presentation

Sublingual tablets containing asenapine

Drugs List

Therapeutic Indications

Uses

Treatment of manic episodes associated with bipolar disorder

Treatment of moderate to severe manic episodes associated with bipolar I disorder in adults.

Dosage

Adults

Contraindications

Children under 18 years
Breastfeeding
Renal impairment - creatinine clearance below 15ml/minute
Severe hepatic impairment

Precautions and Warnings

Family history of long QT syndrome
Patients over 65 years
Predisposition to hypotension
Cardiovascular disorder
Cerebrovascular disorder
Dementia
Diabetes mellitus
Epileptic disorder
History of seizures
Moderate hepatic impairment
Parkinson's disease
Pregnancy

Patients at risk of suicide should be closely supervised
Advise ability to drive/operate machinery may be affected by side effects
Advise patients not eat immediately after a dose
Monitor ECG in patients at risk of QT prolongation
Monitor patients with existing or tendency towards diabetes mellitus
Neonate exposed in utero: Monitor neonate for adverse effects
Advise patient to report unexplained fever, sore throat, bruising, bleeding
Consider discontinuation if signs of tardive dyskinesia occur
Dysphagia & aspiration:caution in patients at risk for aspiration pneumonia
May cause postural hypotension especially in elderly
May impair ability to reduce core body temperature
Discontinue if patient develops neuroleptic malignant syndrome
Advise patient to avoid alcohol during treatment

Elderly patients with psychosis related to dementia, treated with antipsychotic substances, are at an increased risk of death.

Patients with Parkinson's disease or dementia with Lewy Bodies are at increased risk of Neuroleptic Malignant Syndrome and increased sensitivity to antipsychotics.

Pregnancy and Lactation

Pregnancy

Use asenapine with caution in pregnancy.

Use of asenapine during pregnancy is recommended by the manufacturer only if the benefits to the mother outweigh the potential risk to the foetus. There are no adequate data from the use of asenapine in pregnant women.

In animal studies asenapine did not impair fertility in rats and was not found to be teratogenic in rats and rabbits. Embryotoxic effects were, however, found in reproduction toxicology studies using rats and rabbits and asenapine caused mild maternal toxicity and slight retardation of foetal skeletal development.

Neonates exposed to antipsychotics during the third trimester of pregnancy are at risk of adverse reactions. Monitor neonates carefully for extrapyramidal and/or withdrawal symptoms.

The use of all medication in pregnancy should be avoided whenever possible; particularly in the first trimester. Non-drug treatments should also be considered. When essential, a medication with the best safety record over time should be chosen, employing the lowest effective dose for the shortest possible time. Polypharmacy should be avoided. Teratogens taken in the pre-embryonic period, often quoted as lasting until 14-17 days post-conception, are believed to have an all-or-nothing effect. Where drugs have a short half-life, and when the date of conception is certain, this may allow women to be reassured where drug exposure has occurred within this time frame. Further advice may be available from the UK National Teratology Information Service (NTIS) and through ToxBase, available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).

Lactation

Asenapine is contraindicated while breastfeeding.

Studies in rats have shown asenapine to be excreted in milk during lactation. It is not known if asenapine or its metabolites are excreted in human milk.

Neonates, infants born prematurely, those with low birth weight, those with an unstable gastrointestinal function or who have serious illnesses may require special consideration. For any infant, if a drug is prescribed to the nursing mother, it should be at the lowest practical dose and for the shortest time. When drug administration is unavoidable and breastfeeding is to continue, minimisation of exposure of the infant to the drug may sometimes be achieved by timing the maternal doses to just after a feeding episode. Infants exposed to drugs via breast milk should be monitored for unusual signs or symptoms. Interactions between the drug received by the infant from the mother's milk and medication prescribed for the infant should also be considered, for example, when the drug given to the infant may prevent metabolism of the drug received via breast milk.
Specialist advice is available from the UK Drugs in Lactation Advisory Service at https://www.midlandsmedicines.nhs.uk/content.asp?section=6&subsection=17&pageIdx=1

Counselling

The sublingual tablet should be placed under the tongue and allowed to dissolve completely. The tablet will dissolve in saliva within seconds. The sublingual tablets should not be crushed, chewed or swallowed.

Advise the patient to avoid eating and drinking for 10 minutes after administration.

If using in combination with other medication then asenapine should be taken last.

Advise the patient to avoid alcohol.

Advise patient to report unexplained fever, sore throat, bruising or bleeding.

Advise the patient not to drive or operate machinery if affected by certain side effects of asenapine such as sleepiness.

Side Effects

Akathisia
Allergic reaction
Amenorrhoea
Anaphylactic reaction
Angioedema
Anxiety
Bundle branch block
Dizziness
Dysarthria
Dysgeusia
Dyskinesia
Dysphagia
Dystonia
Exacerbation of diabetes
Extrapyramidal effects
Fatigue
Galactorrhoea
Glossodynia
Gynaecomastia
Hyperglycaemia
Hyperprolactinaemia
Hypersalivation
Hypersensitivity reactions
Hypotension
Increased appetite
Increases in hepatic enzymes
Mouth inflammation
Muscle rigidity
Nausea
Neuroleptic malignant syndrome
Neutropenia
Oral hypoaesthesia
Oral mucosal blistering
Oral paraesthesia
Oral ulceration
Orthostatic hypotension
Parkinsonism
Prolongation of QT interval
Pulmonary embolism
Restless legs
Rhabdomyolysis
Sedation
Seizures
Sexual dysfunction
Sinus bradycardia
Sinus tachycardia
Somnolence
Syncope
Throat swelling
Tongue swelling
Visual disturbances
Weight gain

Overdosage

It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.

The following number will direct the caller to the relevant local centre (0844) 892 0111

Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).

Further Information

Last Full Review Date: June 2013

Reference Sources

British National Formulary, 65th Edition (March - September 2013) Pharmaceutical Press, London.

Martindale: The Complete Drug Reference, 37th edition (2011) ed. Sweetman, S. Pharmaceutical Press, London.

Summary of Product Characteristics: Sycrest 5mg sublingual tablets & Sycrest 10mg sublingual tablets. Lundbeck. Revised February 2013.