Cocaine

Drug #196

Cocaine is an alkaloid. Chemically Cocaine is benzoylmethylecgonine. Cocaine is a cerebral stimulant and increases the alertness and helps stay awake. It has been used for atleast 1200 years in custom of chewing coca leaves by natives of the South American Andes. It was isolated as the active material in 1844 from Brazikian coca leaves by Gaedken, which for many years was the only source of it. At present the alkaloid is obtained from Java coca leaves. its anesthetic properties, especially its topical anesthetic action were discovered in 1870s and 1880s. its sole clinical use is as a local anesthetic. It readily enters the central nervous system and produces an amphetamine like effects that is short lasting and more intense. Cocaine is a very heavily abused drug because it can be smoked, snorted or injected for rapid onset of effect.

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Primary Characteristics

It is of Natural origin and belongs to Tropane.

It belongs to Amine uptake inhibitor pharmacological group on the basis of mechanism of action and also classified in Local Anesthetics pharmacological group. It is also classified under Dermatological Products .

Molecular Weight: 303.4 · pK_a: 5.59 · Solubility in Water: 1 in 625 · Solubility in Alcohol: 1 in 6.6 · Non-proprietary name: Cocaine · pH: 4.4 · Isotonic value: 6.33.

Pharmacokinetics

Distribution: Cocaine has a volume of distribution is 84-179 litre. plasma protein binding is 91%.

Elimination: it is metabolised via 90% via liver & serum, plasma half-life is 0.75-1 hr, renal excretion is major.

Indications

Cocaine is primarily indicated in conditions like Cluster headache, Local anaesthesia, Local anaesthetic, Pain, Surface anaesthetic.

Contraindications

Cocaine is contraindicated in conditions like Opthalmologic anaesthesia.

Dosage

Cocaine's dosage details are as follows:

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
12.5 %	12.5 %	—	Topical	As Required
Paediatric Dosage (20kg)
0 – 0	—	—	—	Not Recommended in this Age Group
Neonatal Dosage (3kg)
0 – 0	—	—		Not recommended in this age group

Drug Interactions

Unknown9 interactions

3 interactions

Major1 interaction

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

Cocaine in overdosage may give rise to further complications which include Tachycardia , Myocardial ischemia, Paranoia , Muscle twitching , Acute anxiety reactions , High blood pressure , Psychological dependence.

The signs and symptoms that are produced after acute overdosage of Cocaine are Tachycardia , Hypertension, Ventricular arrhythmias, Medullary stimulation, Skin pallor, Clonic seizures.

Cocaine is known to cause more or less tolerable side effects which are usually transient. These include Hallucination , Hyperactivity, Irritability, Lassitude , Paranoid ideation, Repetitive behaviour patterns.

Warnings / Precautions

Avoid cocaine in patient with known hypersensitivity. It should be given with caution to the elderly, to debilitate, to children, patients with epilepsy, impaired cardiac conduction or respiratory function, shock or liver damage. The application of local anesthetics to the skin for prolonged period or to the extensive area should be avoided. Cocaine should not be applied to damage mucosa. Ophthalmic preparation of cocaine should not be applied to the eyes for prolonged period, because cause the damage of cornea. Patients receiving cocaine for surface anesthesia should be monitored for possible cardiovascular effects. It is not recommended for use during pregnancy.

Interference in Pathology

Cocaine may interfere in the diagnosis of Frings TLC Method of measuring urinary alkaloids .

Available Brands

None recorded.

Storage Conditions

Cocaine should be stored Topical Soln, Nasal Spray .

Drug Classification

1.1.2 — Local anesthetics