CHEARS

What is Modafinil?

• Modafinil is a newer psychostimulant

• It is popular with night-shift workers, who want to improve their alertness and keep them awake.

• This drug will decrease sleepiness and fatigue.

• It will increase the attention span.

• This drug will improve accuracy.

What is the approved indication of Modafinil?

• Day time sleepiness due to narcolepsy

• Sleep apnoea syndrome

• Shift- work disorder (SWD)

What is the other indication of Modafinil?

• Reduce → Euphoria produced by cocaine

• Suppress→ Cocaine withdrawal symptoms

• Prevent→ Relapse of cocaine dependence

What category does Modafinil belong to?

Psychostimulant

How does Modafinil work?

Modafinil inhibits noradrenaline (NA) and Dopamine (DA) uptake and also alters the junctional concentration of glutamate and GABA. The exact mechanism of action is unknown.

What is the pharmacokinetics of Modafinil?

• Mode of administration: Oral route

• Absorption: maximum plasma concentrations→ 2-4 hours

• Metabolism: Liver (Largely: through amide hydrolysis ), (Lesser: Cytochrome P450 -mediated oxidative pathways)

• Elimination half-life: 15 hours.

Whether the drug will cause dependence?

Dependence on this drug is possible on long-term use.

Can Modafinil be used in pregnancy/ Breast feeding?

Modafinil should be avoided in pregnancy and breastfeeding.

Mention the cautions of modafinil?

• Monitor Blood Pressure(BP) and Heart Rate(HR) in hypertensive patients

• Check ECG before initiation

• History of Depression/Mania

• History of Psychosis

• History of Alcohol and drug abuse

• Discontinue the treatment → if psychiatric symptoms develop

• Discontinue the treatment → if rash develop

What are the adverse drug reactions of modafinil?

• Gastrointestinal disturbances (such as Nausea, Diarrhoea, Constipation, Dyspepsia)

• Dry mouth

• Appetite changes

• Headache

• Abdominal pain

• Tachycardia

• Palpitation

• Anxiety

• Dizziness

• Drowsiness

• Confusion

• Depression

• Asthenia

• Paraesthesia

• Visual disturbances

Less commonly:

• Flatulence

• Vomiting

• Mouth ulcers

• Glossitis

• Dysphagia

• Taste disturbances

• Weight Changes

• Tremor

• Emotional lability

• Decreased libido

• Agitation

• Aggression

• Hyperglycaemia

• Hypertension

• Thirst

• Urinary frequency

• Menstrual disturbances

• Acne

• Sweating

• Pruritus

Rarely:

• Hallucinations

• Mania

• Psychosis

• Multi-organ hypersensitivity reaction

• Stevens-johnson Syndrome

• Toxic Epidermal Necrolysis

Mention the contra-indications of Modafinil?

• Moderate to severe uncontrolled hypertension

• Arrhythmia

• History of Left ventricular hypertrophy (LVH)

• Signs of CNS-stimulant induced mitral valve prolapse

Mention the drug interactions of modafinil?

• Phenytoin (Antiepileptics): Modafinil possibly increases the plasma concentration of phenytoin.

• Bosutinib (Cytotoxics): Modafinil possibly decreases the plasma concentration of bosutinib.

• Oestrogen: Modafinil accelerates the metabolism of oestrogen; therefore leads to reduced contraceptive effect.

• Ciclosporin: Modafinil decreases the plasma concentration of ciclosporin.

Mention the dose of Modafinil?

·     Day time sleepiness due to narcolepsy/Sleep apnoea syndrome: 100-200 mg morning and afternoon.

·  Night shift work: 200 mg → 1 hour before starting night shift.