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DRUGS OF ABUSE

DRUGS OF ABUSE. DR Feziwe Bisiwe Department of Internal Medicine. Case presentation Ms S, 32yr old female referred from Hoopstad for Heroin withdrawal. Has been using heroin,cocaine and alcohol for the past 15 yrs of her life and now she wanted to quit.

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DRUGS OF ABUSE

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  1. DRUGS OF ABUSE DR FeziweBisiwe Department of Internal Medicine

  2. Case presentation Ms S, 32yr old female referred from Hoopstad for Heroin withdrawal. Has been using heroin,cocaine and alcohol for the past 15 yrs of her life and now she wanted to quit. No other chronic medications and not on any other medication. She last used the drugs about 6 hrs prior to admission.

  3. On Examination BP:90/60mmHG, Pulse :62 b/min regular Face flushed ,speech slurred and febrile with a temperature of 37.9 She was agitated,anxious and eager to be helped Fingers had tar stains The rest of examination was essentially normal. ECG: showed sinus rhythm,wide QRS complexes with a prolonged QT time Infection markers were all normal FBC: Macrocytosis

  4. LFTs :slightly Raised levels of GGT • HIV: Non –reactive • The rest of blood results were normal. • A diagnosis of Drug withdrawal was made and the patient was admitted and was managed according to the detoxification guidelines. • She made a dramatic improvement but on a third day she absconded.

  5. DRUGS OF ABUSE

  6. Common drugs of abuse • Opioids- mostly heroin • Cocaine • Amphetamines • Prescription meds- mostly benzodiazepines • Codeine containing medications eg Paracodeine and cough mixtures.

  7. HEROIN • Is an opioid- it mimics endorphins • It can either be injected IV, IM, smoked or sniffed. • Effect :IV: 7-8sec,IMI-5-8min,Smoked/sniffed-10-15 min. • It comes as a white powder in its pure forms but with mixing with glucose, talcum and brick dust it ends up as a brownish powder. • The threshold for development withdrawal symptoms on discontinuation or toxicity depends on the tolerance of each patient.

  8. Mechanism of action

  9. The BBB permeability to heroin is about 10 times that of morhpine. • It is hydrolysed into 6-acetylmonomorphine and morphine which then binds to the mu opioid receptors. • This results in GABA release inhibition from the nerve terminal, thus reducing the inhibitory effect of GABA on dopaminergic neurons. • The increased activation of dopaminergic neurons and release of dopamine to the synaptic cleft results in a sustained activation of the post-synaptic membrane.

  10. EFFECTS CNS CVS Increases parasympathetic Bradycardia Hypotension Brady arrhythmias Prolonged QT time Non cardiogenic pulmonary oedema. • Euphoric rush • Analgesic • Anxiolytic • Slow breathing • Sedation • Dependence and addiction

  11. GIT and other effects • Nausea and vomiting • Constipation • Dry mouth • Bacterial infections and infective endocarditis • Pupillary constriction • High energy followed by psychomotor retardation.

  12. WITHDRAWAL SYMPTOMS SIGNS High BP Tachycardia Lacrimation Dilated pupils Piloerection Rhinorrhea Muscle spasms Vomiting and diarrhoea • ‘flu-like symptoms • Abdominal cramps • Anxiety,irritability • Cravings • Fever and chills • Muscle cramps • Nausea,sweating • Restlessness

  13. Heroin Detoxification • Methadone- opioid agonist • Should be started 8-12 hrs after last use • Start with a dose enough to alleviate withdrawal signs without causing toxicity ,then taper it down gradually. • Symptomatic treatment • Alternative drug-Buprenorphine-Naloxone combination • Clonidine-for migraine.

  14. Mx of heroin toxicity • Usually activated charcoal and gastric lavage are not beneficial • Golytely 2l/hr until stools are watery is used to irrigate the bowel. • Naloxone is the definite drug of choice-40mg in 1l N/S or DW @ 10ml /hr. • Pulmonary edema- usually resolves in 24-48 hrs, it only requires supportive Rx. • Convulsions are not common-Benzodiazepines • Rhabdomyolysis-crystalloids and diuresis.

  15. COCAINE • Derived from a coca plant,is a crystalline tropane alkaloid. • It come as an off- white powder or ‘rock’ • It modifies the action of dopamine in the brain by inhibiting its re-uptake from the synaptic cleft and thus causing prolonged postsynaptic stimulation. • Mostly act on the ‘reward pathway 'which consists of ventral segmental area, nucleus accumbens and caudate nucleus, that is why it has a strong potential of psychological dependence.

  16. It also blocks norepinephrine transporter ; serotonin transporter and sodium channel thereby interfering with propagation of action potentials. • Its effects are potentiated by concurrent alcohol abuse, the mortality rate is increased by 25 %. • It is metabolized in the liver and its metabolites are excreted in the urine.

  17. MECHANISM OF ACTION

  18. EFFECTS CNS CVS Activates sympathetic-vasoconstriction,tachycardia Cathecholamines increase about 5 fold Unpredictable BP Impairment of conduction-WPW syndrome Risk of MIs Accelerated atherosclerosis Myocarditis and DCMO Hypercoagulable states • Euphoria • Convulsions • CVA • Appetite suppression • Hallucinations and delusions • Hyperthermia

  19. Other effects • Hyperkalemia • Hypersensitivity pneumonitis-cough and hemoptysis • Central retinal occlusion and endophthalmitis • Platelet aggregation and increased plasminogen activating factor • Destruction of nasal septum

  20. Withdrawal symptoms are the same as the ones mentioned before. • Detoxification is achieved by tapering the dose used and symptomatic treatment. • Toxicity is also managed symptomatically. • They benefit from beta –adrenergic receptor blockers like Labetalol

  21. Phase I - Early stimulation • CNS findings - Mydriasis, headache, bruxism, nausea, vomiting, vertigo, nonintentional tremor (eg, twitching of small muscles, especially facial and finger), tics, preconvulsive movements, and pseudohallucinations (eg, cocaine bugs) • Circulatory findings - Possible increase in BP, slowed or increased pulse rate (possibly with ventricular ectopy), and pallor • Respiratory findings - Increase in rate and depth • Temperature findings - Elevated body temperature • Behavioral findings - Euphoria, elation, garrulous talk, agitation, apprehension, excitation, restlessness, verbalization of impending doom, and emotional lability

  22. Phase II - Advanced stimulation • CNS findings - Malignant encephalopathy, generalized seizures and status epilepticus, decreased responsiveness to all stimuli, greatly increased deep tendon reflexes, and incontinence • Circulatory findings - Hypertension; tachycardia; and ventricular dysrhythmias (possible), which then result in weak, rapid, irregular pulse and hypotension; and peripheral cyanosis • Respiratory findings - Tachypnea, dyspnea, gasping, and irregular breathing pattern • Temperature - Severe hyperthermia (possible) • Phase III - Depression and premorbid state • CNS - Coma, areflexia, pupils fixed and dilated, flaccid paralysis, and loss of vital support functions • Circulatory - Circulatory failure and cardiac arrest (VF or asystole) • Respiratory - Respiratory failure, gross pulmonary edema, cyanosis, agonal respirations, and paralysis of respiration

  23. THE END!!! 1ST YR ON DRUGS 3 YRS LATER.....

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