Cocaine Hydrochloride Solution is indicated to provide local anaesthesia and vasoconstriction of accessible mucous membranes prior to surgery especially in the oral, laryngeal, and nasal cavities. It should be used only by those skilled in the precautions needed to minimise absorption and the consequent risk of arrhythmias. The dispenser contains only 2. Therefore, a maximal dose of 1. Indications from some studies of medicinal cocaine show that death can ensue from 0.
Some persons have a cocaine idiosyncrasy and death may occur quite suddenly after doses of only 20mg. The patient must be monitored for any s or symptoms of toxicity during and after administration of cocaine. The appropriate treatment must be available and medical equipment must be ready for use at all times. If these patients are given cocaine hydrochloride, higher blood levels result, with a greater risk of drug toxicity. Adrenaline is believed to enhance the toxic effects of cocaine by further increasing the level of circulating catecholamines, and thus should not be used Is there any medical use for cocaine association.
Other sympathomimetic drugs are thus also contra-indicated. Cocaine should be avoided in Porphyria, as it has been shown to be porphyrinogenic in animals or in vitro systems, thus exacerbating the disorder. Cocaine should not be applied to damaged mucosa or open wounds because of the risk of systemic toxicity from enhanced absorption.
Cocaine should be used with caution in patients with hypertension, cardiovascular disease or thyrotoxicosis because the vasoconstriction and tachycardia may reduce cardiac oxygenation while increasing oxygen demand It should also be used with caution in patients with diabetes because cocaine sensitises the person to adrenaline which mobilises glucose and causes blood glucose levels to go out of control.
At high doses cocaine depresses the respiratory centres and thus should be cautiously employed in combination with other respiratory depressants e. The use of cocaine in the elderly is not recommended because of the risk of vasoconstriction and tachycardia.
Cocaine is also not recommended in children, or in pregnancy or lactation. Overall, the patient's condition, the appropriate dose and method of administration must all be considered prior to the application of cocaine. The initial s and symptoms of cocaine toxicity and the appropriate treatment required to combat toxicity must be known to the surgeon or anaesthetist. Ecothiopate eye drops for the treatment of Glaucoma, and neostigmine for the treatment of Myasthenia Gravis.
If these drugs are administered to patients receiving cocaine, higher blood levels result, with a greater risk of drug toxicity. See Contra-indications. Adrenaline is believed to enhance the toxic effects of cocaine by further increasing the level of circulating catecholamines.
A review of the history, actions, and legitimate uses of cocaine
Ephedrine is used in the treatment of reversible airways obstruction and is present in some cough linctus preparations. Amphetamines CNS stimulants have some similar actions to sympathomimetics. Cocaine potentiates the effects and toxicity of MAO inhibitors, e.
These drugs also increase the activity of the Sympathetic Nervous System, which is also increased by administration of cocaine. Maintenance of anaesthesia with halothane, a volatile anaesthetic agent, may augment any interaction between cocaine and catecholamines by sensitising the myocardium.
However, deeper levels of general anaesthesia inhibit adrenal release of catecholamines and may conversely decrease the potential arrhythmogenic effects. Cocaine exposure early in pregnancy is reflected by cocaine and metabolite burden in the meconium, which is initially formed at the end of the first trimester, due to cocaine crossing the placenta. Animal and autopsy studies indicate that the cocaine metabolite benzoylecgonine preferentially accumulates in foetal tissue. Recent human and animal studies suggest that the slowly eliminated metabolites of cocaine have ificant physiological and behavioural properties.
There is also an increased risk of spontaneous abortion and other birth complications due to vasoconstriction by cocaine increasing maternal blood pressure and reducing placental blood flow. The following s and symptoms are typical of babies born following cocaine use by the mother during pregnancy : irritability, inconsolability, hypertoxicity, tremulousness, hyperactive moro reflex, sneezing or yawning, lethargy, suck reflex, high pitched cry, poor feeding, poor weight gain, fever, diarrhoea, spitting Is there any medical use for cocaine vomiting, tachypnoea, tachycardia, skin abrasions and respiratory distress.
Cocaine is also excreted in breast milk.
Due to the pharmacological actions of cocaine, it is recommended that patients who have been administered cocaine do not drive or operate machinery. This medicine can impair cognitive function and can affect a patient's ability to drive safely. This class of medicine is in the list of drugs included in regulations under 5a of the Road Traffic Act When prescribing this medicine, patients should be told:.
Cocaine may cause restlessness, excitement, euphoria, garrulousness and increased motor activity. With high doses or repeated use, confusion, paranoia, hallucinations, altered tactile sensations and psychosis have been reported. Seizures can occur, perhaps due to lowering of the seizure threshold, or hyperpyrexia, or due to life threatening cardiac arrhythmias.
Cocaine directly causes a rise in body temperature by increasing heat production through stimulated muscle activity, and indirectly by causing vasoconstriction that decreases heat loss. A direct pyrogenic effect may be caused by cocaine's direct effect on thermoregulatory centres in the hypothalamic area. Low doses of cocaine in humans do not change respiratory rate or depth, but at higher doses a CNS mediated increase in respiratory rate and decrease in tidal volume is described.
A review of the history, actions, and legitimate uses of cocaine
A migraine-like headache may be the result of cocaine induced vascular changes. Adrenergic stimulation may cause intensive hypertension, due to tachycardia and peripheral vasoconstriction. Cocaine increases cardiac activity, which raises oxygen demand within myocardial tissue. Other s of adrenergic excess seen with cocaine include mydriasis, diaphoresis, tremor, hyperactive bowel sounds and hyperreflexia.
Vasoconstriction due to cocaine may also produce ischaemia in the fingers, toes, spinal cord, kidneys, spleen, and intestines. In low doses cocaine has an anorexic effect. The s and symptoms of overdose must be known to the otolaryngologist or anaesthetist administering cocaine topically.
Cocaine hydrochloride solution 10% w/v
Toxicity first occurs as an overstimulated excited state. The toxic reaction may progress to convulsions, loss of consciousness, respiratory and cardiovascular depression or arrest, and death. Toxicity may arise from any route of cocaine administration. Clinically, otolaryngologists reported a higher percentage of untoward reactions when cocaine was applied to the tracheobronchial tree rather than the nasal mucosa.
Symptoms of acute toxicity include delirium, tremor, massive convulsions and a direct cardiotoxic effect due to its sympathomimetic effect. Controlled clinical studies have been performed examining the dose-response effects from intranasal snorting administration of cocaine.
At 10mg no observable subjective or physiological effects were apparent; at 25mg there was an increase in systolic blood pressure and mild euphoria reported as relaxation; at mg, heart rate and diastolic blood pressure were increased and a strong feeling of euphoria was present. These effects were short-lasting and lethargy and irritability as an after-effect were reported by a few subjects within one hour after a cocaine administration.
A fatal dose of cocaine is about 0.
This must be emphasised in order to appreciate the potency and danger of this cocaine solution. Cocaine use by pregnant women can interfere with gestation and produce abnormalities, possibly permanent, in their children. See Pregnancy And Lactation. At clinical doses, cocaine has little general toxicity, when applied locally and for a short period of time. If a cocaine-impregnated pledget is still in the nose when toxicity occurs, it must be promptly removed.
Seizures, and cardiovascular and respiratory collapse in the late stages have been treated with respiratory support, anti-convulsants, and cardiotonic drugs. The treatment of acute poisoning by cocaine should include the removal of any remaining drug from the mucosal surface by rinsing with tap water or normal saline.
In a medical setting where cocaine is used, positive-pressure breathing equipment should be functional and easily accessible, and intravenous diazepam should be immediately available. Intravenous pentobarbital is a more stable preparation; it is slower acting but can be used if diazepam is not available. Delusions may respond to neuroleptics phenothiazine and butyrophenone but these agents also may increase the chance of seizures; benzodiazepines may be useful in reducing anxiety.
This drug produces its local anaesthetic effects by inhibiting the permeability of the cell membrane to sodium ions during depolarisation, thus blocking the initiation and conduction of electrical impulses within nerve cells.
Position statement: medical use of cocaine
Its actions on the central nervous system involve the alteration of several neurotransmitters. Cocaine affects the sympathetic nervous system by blocking the re-uptake of noradrenaline and dopamine. This initially causes cortical stimulation and may result in restlessness, excitement, euphoria, garrulousness, and increased motor activity. Confusion, paranoia, hallucinations, altered tactile sensations, and psychosis have also been reported, especially with high doses or repeated use.
Position statement: medical use of cocaine
Seizures can occur, perhaps due to lowering of the seizure threshold, due to cocaine-induced hyperpyrexia, or due to life threatening cardiac arrhythmias. Respiratory Effects:- Cocaine initially stimulates the respiratory centre, resulting in increased respiratory rate.
However, the depth of respiration is soon decreased to a rapid and shallow pattern. This may be followed by depression of the medullary centres, causing respiratory failure. Cocaine's effects on the lungs and respiration can also result in metabolic acidosis or alkalosis.
The respiratory effects of Cocaine appear to be dose related. Low doses in humans do not change respiratory rate or depth, but at higher doses a CNS mediated increase in respiratory rate and decrease in tidal volume is described. At very large cocaine doses, Cheyne-Stokes respirations and apnoea occur.
Cerebrovascular effects:- Cocaine can reduce blood flow within the brain. Other complications include cerebral haemorrhage or infarction, most likely related to sudden intensive hypertension resulting from adrenergic stimulation. In the central nervous system, cocaine suppresses both rapid eye movement REMsleep and total sleep. In low doses, cocaine has an anorexic effect.