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Cocaine produces anesthesia by inhibiting excitation of nerve endings or by blocking conduction in peripheral nerves. This is achieved by reversibly binding to and inactivating sodium channels. Sodium influx through these channels is necessary for the depolarization of nerve cell membranes and subsequent propagation of impulses along the course of the nerve. When a nerve loses its ability to propagate an impulse, the individual loses sensation in the area supplied by the nerve. Cocaine also has a profound effect on the CNS. Cocaine blocks reuptake of dopamine in the midbrain region responsible for reward mediation. This leads to increased stimulation and a sense of euphoria and arousal. As the cocaine level decreases, so does the dopamine level in this region, resulting in depression and a craving for the drug. Cocaine also blocks the reuptake of norepinephrine in the sympathetic portion of the autonomic nervous system, resulting in increased stimulation of the sympathetic nervous system. This results in the characteristic tachycardia, hypertension, diaphoresis, mydriasis, and tremors associated with cocaine use. Cocaine is the only local anesthetic with vasoconstrictive properties. This is a result of its blockade of norepinephrine reuptake in the autonomic nervous system.
Cocaine is absorbed rapidly through mucous membranes, and peak plasma levels (ie, 20-474 ng/mL) are reached within 15-60 minutes. Half-life in serum is 30-90 minutes. Cocaine is metabolized in several ways. Hydrolysis by plasma pseudocholinesterases accomplishes the majority of cocaine degradation to benzoylecgonine and ecgonine methyl ester. Oxidative metabolism in the liver produces norcocaine, a toxic substance capable of causing severe hepatic damage. Approximately 5% of absorbed cocaine is excreted in the urine unmetabolized. Cocaine is detectable in the nasal mucosa for 3 hours following application. Serum and urine levels are measurable for approximately 6 hours following application.
Cocaine is used for topical anesthesia and vasoconstriction for surgery of the nose, throat, and oral cavity. Cocaine provides rapid and profound anesthesia in conjunction with vasoconstriction and decongestion of swollen mucosa. Cocaine hydrochloride is available commercially in the United States as flakes, crystals, 135-mg tablets, and solutions of various concentrations. The flakes and crystals are intended for application via moistened cotton swabs. The tablets are to be used in preparation of a topical solution. The premade topical solutions are available in strengths ranging from 2-10%. The safe maximum dosage is reported to be 200 mg or 2-3 mg/kg. However, even 200 mg can cause adverse reactions if rapidly absorbed. Spraying or painting cocaine on the intended surgery site causes more rapid absorption than application by patch or pledget. Clinical studies have shown that only approximately one third of a cocaine solution placed on pledgets is absorbed via the nasal mucosa, providing an added margin of safety for the surgeon. When epinephrine is added to the solution to promote further vasoconstriction, systemic absorption decreases; however, according to published series, the decrease is inconsistent. Late absorption of cocaine has also been reported when cocaine is administered with epinephrine. Therefore, the use of epinephrine cannot be assumed to protect from systemic cocaine absorption. The addition of epinephrine has also been reported to enhance the sympathomimetic action of cocaine, causing hypertension and tachyarrhythmias. To use cocaine in the nasal cavity, cotton pledgets are soaked in the cocaine solution. After being wrung out, the pledgets are introduced into the operative field with bayonet forceps. Pay particular attention to placing the pledgets in contact with the mucosal surface. After the pledgets have been in place for at least 10 minutes, they may be removed from the side to be approached first. Infiltration of submucosal lidocaine with epinephrine may then be performed. This is best performed with a small syringe and 25-gauge or smaller needle. Proper placement creates blanching of the mucosa. Rarely is more than 1.5 mL required for each side. After allowing several minutes for the injected solution to take effect, inspect the mucosa for the anticipated vasoconstriction. If the patient reports pain at this time or further along in the operative course, pledgets may be loosely reapplied. Another more recently developed use of cocaine is in combination with tetracaine and adrenaline (TAC), composed of 0.5% tetracaine, epinephrine 1:200,000, and 11.8% cocaine. This combination has been used in the pediatric population for suturing lacerations less than 10 cm long in the emergency department. It has been found to be most effective in the head, neck, and scalp; less effective in the trunk; and ineffective in the extremities. A few drops of the solution may be placed directly on the wound, or, preferably, a moistened cotton ball soaked in the solution may be applied to the wound. Constant gentle pressure is then applied to the cotton balls for 10-20 minutes. After testing the adequacy of anesthesia, the wound may be irrigated, cleansed, and sutured. Inadequacy of anesthesia is remedied by injection of local anesthetic. Monitor the patient with pulse oximetry and telemetry during use of TAC. In addition, observe the patient for any signs or symptoms of systemic toxicity. Following application and suturing, observe the patient for an additional 60 minutes to ensure that no untoward effects of cocaine absorption occur. The benefits of TAC include ease of application, patient comfort during application, and avoidance of wound distortion from the injection of local anesthetic solution. This technique has been proven safe and effective in numerous published studies and is gaining wide popularity among emergency departments. TAC should not be used on mucous membranes, burns, or large abrasions because of the risk of rapid absorption and systemic toxicity.
Although adverse reactions to cocaine seldom occur in the medical field, those that do may be rapid, unexpected, and severe. Other good alternatives for anesthesia are available, and many surgeons have ceased using cocaine because of its unpredictable effects and the risk of having such a highly addictive drug in the office. Cocaine toxicity may have profound adrenergic effects on the CNS, cardiovascular system, and respiratory system. Sympathetic stimulation of the cardiovascular system may lead to hypertension, tachycardia, ventricular fibrillation, and cardiac arrest. Other serious complications include direct cardiotoxicity, angina, myocardial infarction, cerebrovascular accident, transient ischemic attack, pulmonary edema, hepatotoxicity, intestinal ischemia, seizures, and CNS depression. Cocaine readily passes into breast milk and across the placenta, an important consideration in patients who are pregnant or nursing. Stillbirth, preterm labor, and abruptio placentae may occur. Intrauterine growth is also restricted. These often-profound effects on the fetus may continue after birth. Developmental delay is common in children born to mothers with cocaine in their system.
The cornerstone of treatment for cocaine toxicity is early recognition and action. The treating physician must curtail the operative procedure and remove any remaining pledgets. Immediately activate advanced cardiac life support protocols, including intubation and defibrillation if indicated. Above all, seek help immediately. In a hospital setting, assistance is readily available. In the office surgery setting, call emergency services (ie, dial 911 in the United States) immediately. The surgeon must direct resuscitation until assistance arrives. This requires that any surgeon using cocaine in the office be familiar with advanced cardiac life support protocols and have the proper equipment on hand should an emergency situation arise. Cocaine toxicity has no known antidote. Aggressive resuscitation is the only treatment. In addition to intubation and defibrillation, administering drugs such as propranolol, nitrates, calcium channel blockers, and alpha-adrenergic blockers may be necessary in an attempt to improve coronary blood flow and restore normal sinus rhythm. Control seizure activity with diazepam (Valium), and aggressively treat hyperthermia with cooling blankets.
Action, Medical Uses, and Dosage.-
In large doses, coca is said to cause delirium, hallucination, and finally cerebral congestion. In medium doses it acts as a stimulant, increasing the temperature of the body, as well as the respiration and frequency of the pulse; in a moderate dose it excites the nervous system in such a manner as to render the performance of muscular exertion much easier, and producing a sensation of calmness. According to Dr. Mantegazza, its use has produced an erythematous eruption resembling pityriasis, with a sense of prickling and itching; the intoxication produced by it, differs from that resulting from the use of alcoholic drinks, the symptoms being feverishness, increased heat of the surface, palpitation, photopsy, headache, vertigo, increased frequency of the pulse, a peculiar roaring tinnitus, strong desire for active locomotion, with increased sense of strength and agility, exaltation of the intellectual sphere, sense of isolation, followed by a feeling of intense calm and comfort, complete apathy, sleep, odd and rapidly changing dreams, and from which the patient awakes without debility or indisposition of any kind. The leaves of coca, chewed or taken in a weak infusion, stimulate the gastric nerves and greatly facilitate digestion; and are also useful in relieving the sense of fatigue from excessive mental or physical exercise. A drachm of the leaves chewed produces a feeling of comfort in the stomach, and upon repeating the dose a few times, a slight burning sensation is experienced in the mouth and pharynx, with increased thirst, rapid digestion, and a substitution of the coca odor in the stools for that ordinarily present.
More recently, M. Moreno, who made some interesting experiments upon the effects of coca and cocaine, remarks, that coca gives much less arterial tension than coffee, as he has convinced himself with the aid of the sphygmograph. Relatively to its action, M. Weddell has observed: "One of two things, either coca incloses some nutritive principles which directly sustain the forces, or else it simply deceives the hunger, by acting upon the economy as an excitant." M. Moreno has submitted animals to an insufficient alimentation or to absolute inanition, and in these conditions be has observed that those to whom he administered coca lost more of their weight and died more speedily. He concludes that if coca sustains the forces, that is to say, permits man to forget hunger, it is not, however, as an aliment, and does not succeed in satisfying it. He has carefully studied the special action exerted by this substance upon the nervous system. According to him it determines (1) phenomena which place it with strychnine (tetanic and spontaneous convulsions, and, upon the least excitation of the animals, death); (2) in a small dose, it provokes a remarkable excitation of sensibility, dilatation of the pupil, irregularity of the movements; the animals seem to have lost the coördinating power of their movements. Lastly, in large doses, it causes a diminution, followed by exhaustion, of sensation, without motility being completely abolished, and in all the cases, the pupils remain dilated. Like tea and coffee, coca lessens the elimination of urea, acting thereby indirectly as a food, though not a food in itself. That hunger is staved off by it is probably due to a benumbing effect upon the nervous supply of the stomach.
That the habit of using coca will grow upon one, is illustrated by its effects upon the mountaineers of the Peruvian Andes (see History), who employ it to lessen fatigue, and to guard against the pulmonary hemorrhage likely to occur at high altitudes. The habitual coca-chewer acquires a general apathetic state and his step becomes uncertain. Deep purplish circles surround big sunken eyes, his lips tremble, a peculiar blackish colorization is observed at the angles of the mouth, the teeth become green and encrusted, and an intolerably offensive odor is imparted to the breath. Extreme emaciation, with intractable sleeplessness, and anasarca ensue and finally death completes the destruction.