NAME OF DRUG

Generic name: Methotrimeprazine

Brand name: nozinan

Classification: Antipsychotics

ATC Classification

N05AA02 - levomepromazine ; Belongs to the class of phenothiazine antipsychotics with aliphatic side-
chain.

Regulatory Classification

Rx

Presentation/Packing

Tab 25 mg x 100's. 100 mg x 100's.

MODE OF ACTION

Nozinan possesses antiemetic, antihistamine and antiadrenaline activity and exhibits a strong sedative
effect.

Pharmacology: Nozinan potentiates the action of other central nervous system (CNS) depressants but
may be given in conjunction with appropriately modified doses of narcotic analgesics in the
management of severe pain. Nozinan does not significantly depress respiration and is particularly useful
where pulmonary reserve is low.

Pharmacokinetics: Maximum serum concentrations are achieved in 2-3 hrs. Excretion is slow, with a t½
of about 30 min. It is eliminated via urine and feces.

INDICATION

Management of terminal illness particularly in those marked by restlessness, anxiety, agitation,

emotional disturbance, pain, nausea and vomiting.

In psychiatry, especially in schizophrenia when it is desirable to reduce psychomotor activity.

DOSAGE

Adults: Ambulatory Patients: Initially, the total daily oral dose should not exceed 25-50 mg, usually
divided into 3 doses; a larger portion of the dosage may be taken at bedtime to minimize diurnal
sedation. The dosage is then gradually increased to the most effective level compatible with sedation
and other side effects.
Bed Patients: Initially, the total daily oral dosage may be 100-200 mg, usually divided into 3 doses,
gradually increased to 1 g daily if necessary. When the patient is stable, attempts should be made to
reduce the dosage to an adequate maintenance level.

Children: Children are very susceptible to the hypotensive and soporific effects of levomepromazine. It is
advised that a total daily oral dosage of 40 mg should not be exceeded. The average effective daily
intake for a 10-year old is 15-20 mg.

Overdosage

Symptoms: Symptoms of levomepromazine overdosage include drowsiness or loss of consciousness,

hypotension, tachycardia, electrocardiogram (ECG) changes, ventricular arrythmias and hypothermia.
Severe extrapyramidal dyskinesias may occur.

Treatment: If the patient is seen sufficiently soon (up to 6 hrs) after ingestion of a toxic dose, gastric
lavage may be attempted. Pharmacological induction of emesis in unlikely to be of any use. Activated
charcoal should be given. There is no specific antidote. Treatment is supportive.

CONTRAINDICATIONS

There are no absolute contraindications to the use of Nozinan in terminal care.

Special Precautions

Nozinan should be avoided or used with caution in patients with liver dysfunction or cardiac disease.

The hypotensive effects of Nozinan should be taken into account when it is administered to patients
with cardiac disease and in the elderly or debilitated. Patients receiving large initial doses should be kept
in bed. Avoid alcoholic drinks.

Effects on the Ability to Drive or Operate Machinery: Nozinan may cause drowsiness, disorientation,
confusion or excessive hypotension which may affect patient's ability to drive or operate machinery.

Use in pregnancy: Safety in pregnancy has not been established.

Use in the elderly: It is not advisable to give Nozinan to ambulatory patients >50 years unless the risk of
hypotensive reaction has been assessed.

Use In Pregnancy & Lactation

Use in pregnancy: Safety in pregnancy has not been established.

SIDE EFFECTS

Somnolence and asthenia are frequent side effects. Dry mouth is encountered occasionally. Hypotension
may occur, especially in elderly patients. A rise in ESR may occasionally be encountered. Agranulocytosis
has been reported, as have photosensitivity and allergic skin reactions.
Parkinson-like reactions may occur in patients receiving prolonged high dosage. Jaundice is rare side
effect. Other adverse effects common to phenothiazine neuropleptics may be seen.

Drug Interactions

Simultaneous administration of desferrioxamine and prochlorperazine has been observed to induce a

transient metabolic encephalopathy characterized by loss of consciousness for 48-72 hrs. It is possible
that this may occur with levomepromazine since it shares many of the pharmacological activities of
prochlorperazine. Adrenaline must not be used in patients overdosed with neuroleptics.

Storage

Store at temperatures not exceeding 30°C.

NURSING RESPONSIBILITIES

Carefully supervise ambulation for at least 6 h, but preferably 12 h. Orthostatic hypotension with
faintness, weakness, and dizziness may occur within 10–20 min after drug administration and may last
4–6 h and occasionally as long as 12 h. Tolerance to effects usually develops with successive doses.

Excessive sedation and amnesia also occur commonly during early drug therapy.

Assess BP and pulse frequently until dosage requirements and response are stabilized. Monitor older
adult and debilitated patients closely.

Methotrimeprazine injection contains a bisulfite, an allergen for some patients.

Do not treat severe hypotension with epinephrine; it is specifically contraindicated.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold;
classifications in SMALL CAPS; Canadian drug name; Prototype drug