Cocaine

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.

Brands
Adult Dose
Dose: 5 to 20 %
Single Dose: 12 (12.5)
Frequency: As recommended.
Route: Topical
Instructions: As Required
Neonatal
Dose:
Single Dose:
Frequency:
Route:
Instructions: Not recommended in this age group
Paedriatic
Dose:
Single Dose:
Frequency:
Route:
Instructions: Not recommended in this age group
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 Dermatological Products and Local Anesthetics pharmacological group.The Molecular Weight of Cocaine is 303.40. It is weakly acidic drug, 6.33% solution of the drug is isotonic and Its pKa is 5.59.
Contraindications
Cocaine is contraindicated in conditions like Opthalmologic anaesthesia.
Effects
The severe or irreversible adverse effects of Cocaine, which give rise to further complications include Tachycardia, Acute anxiety reactions, High blood pressure, Paranoia, Muscle twitching, Psychological dependence, Myocardial ischemia.The signs and symptoms that are produced after the acute overdosage of Cocaine include Tachycardia, Hypertension, Skin pallor, Ventricular arrhythmias, Medullary stimulation, Clonic seizures.The symptomatic adverse reactions produced by Cocaine are more or less tolerable and if they become severe, they can be treated symptomatically, these include Irritability, Hallucination, Hyperactivity, Paranoid ideation, Lassitude, Repetitive behaviour patterns.
Indications
Cocaine is primarily indicated in conditions like Cluster headache, Local anaesthesia, Local anaesthetic, Pain, Surface anaesthetic.
Interactions
Cocaine is known to interact with other drugs, the details of drug interactions is as follows:DrugDetailsSeverityOnsetManagementAdrenalineCoadministration can result in life threatening cardiac arrhythmias.MajorUse this combination with extreme caution.AlcoholAmisulprideEnhanced hypotensive and sedative effects when Amisulpride given with opioid analgesic (e.g Cocaine).CannabisGuanethidineHalothaneMethotrimeprazine (Maleate)Noradrenaline (Acid Tartrate)Promazine (HCl)SulpirideSuxamethonium (Cl)VORICONAZOLEVoriconazole may increase the serum concentration of cocaine by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of cocaine if voriconazole is initiated, discontinued or dose changed.Vortioxetineincreases the level of vortioxetinemonitor closely, use alternative or decrease dose by 50% when coadministered These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Interfrence
Frings TLC Method of measuring urinary alkaloids
Risks
Drug should not be given to Paediatrics, Pregnant Mothers, Cardiac / Hypertensive Patients, Geriatrics, and Neonates.If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.
Storage
Topical Soln, Nasal Spray Store Below 25°C. Protect from Sunlight.
Warnings
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.
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