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Dr. RAGHU PRASADA M S
MBBS,MD
ASSISTANT PROFESSOR
DEPT. OF PHARMACOLOGY
SSIMS & RC.
1
 Taking a Drug for any reason
other than a medical one…
 To get a feeling of
euphoria (high)
2
 uncontrollable compulsive drug
seeking and use, even in the face of
negative health and social
consequences.”
 Results from both psychological and
physical dependence on the drug
3
 Treatment of withdrawal symptoms
 Aversion therapy
 To reduce craving
 To prevent relapse
 Rehabilitation & psychosocial
intervention
4
Single agent
Acamprosate
 Naltrexone
 Disulfiram
 Aimed at complete abstinence ,
can be started at any time
including withdrawal phase,
 may be started immediately
during first consultation
 Early onset with family loading,
helps in heavy drinking and may be
choice in which acamprosate trial has
failed,
 Liver function test is mandatory
 Patient completely motivated and
with good social support, still low
acceptability
 SSRIs (Fluoxetine,
Sertraline, Citalopram)
 Topiramate
 Baclofen
 Effective with co morbid
depression
 Can be used as single
agent, or with co
morbidities like seizure,
bipolar disorder.
 Helpful in withdrawal
management and relapse
prevention in patients with
cirrhosis liver. Also co
morbid cannabis or solvent
or benzodiazepine uses
6
General principles of treatment
 Careful monitoring and supportive care
 Ample fluids (p/o or IV fluids if
dehydrated)
 Correction of electrolyte imbalance
 Parenteral Thiamine(100 mg p.o or i.v or
i.m) daily
 Restrict access to addicting substances
 Involve significant others in the treatment
from the initial stages
 Liaise with specialists as appropriate
7
 Cross tolerant medications with alcohol
 Benzodiazepines
 Diazepam and Chlordiazepoxide
Lorazepam and oxazepam - short acting
(patients with liver
problems, in elderly)
 Others (more than 150 agents,
carbamazepine; valproate, ß adrenergic
antagonists etc.,)
 Emerging: Baclofen
8
Ethanol AcetateAcetaldehyde
•Flushing
•Headache
•Palpitations
•Dizziness
•Nausea
ADH ALDH
 .
9
Disulfiram
 Main contraindications:
recent alcohol use, pregnancy, rubber, nickel
or cobalt allergy, cognitive impairment, drug
interactions
hepatitis, neuropathy
10
Disulfiram 250 mg/d-->500 mg/d
Main side effects:
Acamprosate (calcium acetyl homo
taurinate)
 structure similar to GABA amino
acid.
 Restores the GABA activity.
 reduce glutamate surges that
excite NMDA- Rs.
 acts as a neuro-protectant and
protect neurons from damage
caused by alcohol withdrawal
11
The Reward
Pathway
Ethanol
Dopamine
Beta endorphin
release potentiated
Naltrexone-
aimed at reducing the psychological need or craving for alcohol.
prefrontal cortex
nucleus accumbens
VTA
Firing
12
▪ Main contraindication:
opiates, pregnancy
▪ Main side effects:
13
Naltrexone 12.5 mg/d-->25 mg/d-->50 mg/d
▪ a 5-HT3 antagonist that exerts its antidrinking effects
through cortico-mesolimbic dopamine system
modulation.
▪ improve drinking outcomes in patients with early-onset
alcoholism.
▪ Adverse events are mild
▪ starting dosage of 4 mcg/kg twice daily should be
maintained throughout treatment.
14
15
Treatment of
 Dependence and Abuse
 Intoxication
 Withdrawal
16
Naltrexone
 Complete abstinence approach
 long term treatment helps in
maintaining complete abstinence
 extinction of drug seeking behavior
 blocking the effects of opioid over
a significant period
 Reduced craving
Advantage
 No tolerance or
withdrawal
 Not a schedule drug
 No abuse potential
Disadvantage
 Abstinence for 5-7
days
 Retention and
compliance issues
 Sensitivity to over
dosages
18
Methadone
Buprenorphine
LAAM( levo Alfa acetyl methadone)
Advantages
 Best available
evidence
 Lower costs
 Good Retention and
abstinence rates
Disadvantages
 Mortality following
overdose
 Scheduled drug
 Supervised clinic
 Daily dosing
 Abuse and dependence
20
 semi-synthetic opium alkaloid derivative of
thebaine.
 long acting, highly lipophilic opiate
 Mixed agonist antagonist
 Side effects – as in methadone
elevated liver enzymes
 Toxicity – Less risk, none reported
but if occurs, difficult to reverse and needs higher
doses of naloxone
.
21
THANKYOU
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Class deaddiction 2

  • 1. Dr. RAGHU PRASADA M S MBBS,MD ASSISTANT PROFESSOR DEPT. OF PHARMACOLOGY SSIMS & RC. 1
  • 2.  Taking a Drug for any reason other than a medical one…  To get a feeling of euphoria (high) 2
  • 3.  uncontrollable compulsive drug seeking and use, even in the face of negative health and social consequences.”  Results from both psychological and physical dependence on the drug 3
  • 4.  Treatment of withdrawal symptoms  Aversion therapy  To reduce craving  To prevent relapse  Rehabilitation & psychosocial intervention 4
  • 5. Single agent Acamprosate  Naltrexone  Disulfiram  Aimed at complete abstinence , can be started at any time including withdrawal phase,  may be started immediately during first consultation  Early onset with family loading, helps in heavy drinking and may be choice in which acamprosate trial has failed,  Liver function test is mandatory  Patient completely motivated and with good social support, still low acceptability
  • 6.  SSRIs (Fluoxetine, Sertraline, Citalopram)  Topiramate  Baclofen  Effective with co morbid depression  Can be used as single agent, or with co morbidities like seizure, bipolar disorder.  Helpful in withdrawal management and relapse prevention in patients with cirrhosis liver. Also co morbid cannabis or solvent or benzodiazepine uses 6
  • 7. General principles of treatment  Careful monitoring and supportive care  Ample fluids (p/o or IV fluids if dehydrated)  Correction of electrolyte imbalance  Parenteral Thiamine(100 mg p.o or i.v or i.m) daily  Restrict access to addicting substances  Involve significant others in the treatment from the initial stages  Liaise with specialists as appropriate 7
  • 8.  Cross tolerant medications with alcohol  Benzodiazepines  Diazepam and Chlordiazepoxide Lorazepam and oxazepam - short acting (patients with liver problems, in elderly)  Others (more than 150 agents, carbamazepine; valproate, ß adrenergic antagonists etc.,)  Emerging: Baclofen 8
  • 10.  Main contraindications: recent alcohol use, pregnancy, rubber, nickel or cobalt allergy, cognitive impairment, drug interactions hepatitis, neuropathy 10 Disulfiram 250 mg/d-->500 mg/d Main side effects:
  • 11. Acamprosate (calcium acetyl homo taurinate)  structure similar to GABA amino acid.  Restores the GABA activity.  reduce glutamate surges that excite NMDA- Rs.  acts as a neuro-protectant and protect neurons from damage caused by alcohol withdrawal 11
  • 12. The Reward Pathway Ethanol Dopamine Beta endorphin release potentiated Naltrexone- aimed at reducing the psychological need or craving for alcohol. prefrontal cortex nucleus accumbens VTA Firing 12
  • 13. ▪ Main contraindication: opiates, pregnancy ▪ Main side effects: 13 Naltrexone 12.5 mg/d-->25 mg/d-->50 mg/d
  • 14. ▪ a 5-HT3 antagonist that exerts its antidrinking effects through cortico-mesolimbic dopamine system modulation. ▪ improve drinking outcomes in patients with early-onset alcoholism. ▪ Adverse events are mild ▪ starting dosage of 4 mcg/kg twice daily should be maintained throughout treatment. 14
  • 15. 15
  • 16. Treatment of  Dependence and Abuse  Intoxication  Withdrawal 16
  • 17. Naltrexone  Complete abstinence approach  long term treatment helps in maintaining complete abstinence  extinction of drug seeking behavior  blocking the effects of opioid over a significant period  Reduced craving
  • 18. Advantage  No tolerance or withdrawal  Not a schedule drug  No abuse potential Disadvantage  Abstinence for 5-7 days  Retention and compliance issues  Sensitivity to over dosages 18
  • 20. Advantages  Best available evidence  Lower costs  Good Retention and abstinence rates Disadvantages  Mortality following overdose  Scheduled drug  Supervised clinic  Daily dosing  Abuse and dependence 20
  • 21.  semi-synthetic opium alkaloid derivative of thebaine.  long acting, highly lipophilic opiate  Mixed agonist antagonist  Side effects – as in methadone elevated liver enzymes  Toxicity – Less risk, none reported but if occurs, difficult to reverse and needs higher doses of naloxone . 21