Anti-Smoking Drugs

ANTI-SMOKING DRUGS


ANTI-SMOKING DRUGS

Anti-smoking drug Drug category Description & drug details
Varenicline

 

Direct acting nicotinic agonist
  • Have selectivity for α4 β2 isoform of NN receptors.
  • Effective orally; Half-life: 14-20 hr.
  • Adverse effects: 
    • Headache, nausea & sleep disturbances.
Nicotine patch

 

A transdermal patch

 

  • Contains nicotine applied to patient’s body.
  • Nicotine dose is slowly decreased & finally withdrawn.
  • Effective only in 18-20% patients.
Bupropion/Amfebutamone

 

Anti-depressant drug nicotinic receptor antagonist
  • Acts by selectively inhibiting of neuronal reuptake of 5-HT, NE & DA.
  • Advantage:
    • Decreases nicotine craving.
    • Increased efficacy in combining with nicotine patch.
  • Treatment duration
    • 8-10 weeks.
  • Adverse effects: 
    • Can cause CNS stimulation resulting in seizures
  • Contraindicated in epileptic patients.
Clonidine Centrally acting alpha-agonist
  • Very effective drug for reducing nicotine withdrawal effects.
  • Decreases craving.
  • Better than nicotine chewing gum.
  • Recommended in cardiac & insomniac patients.
Rimonabant Cannabinoid receptor antagonist
  • Causes increased 5-HT & dopamine levels.
  • Adverse effects:  
    • Nausea, vomiting, suicidal tendencies (depression) & anxiety.
Topiramate Antagonist at AMPA/kainate receptors of glutamate
  • Used as an anti-smoking drug.
  • Also, causes weight loss.
Nortryptyline Main active metabolite of amitriptyline.
  • Longer t1/2 than parent compound.
  • Produces prolonged abstinence rates as compared to placebo.
  • Adverse effects – 
    • Dry mouth & sedation.
Glucose  
  • Single dose nicotine relieves hunger in smokers.
  • Hunger pains are associated with cigarettes craving.
  • Treatment – 
    • Glucose tablets used to decrease craving.
Mecamylamine Nicotine antagonist
  • Blocks rewarding effects of nicotine.
  • Adverse effect – Constipation.
Tryptophan & high carbohydrate diet Serotonin enhancing substances
  • Reduces nicotine’s withdrawal symptoms.

Exam Important

ANTI-SMOKING DRUGS

  • Nicotine replacement therapy is available in all forms like chewing gum, lozenges, patch, except tablets.
  • Bupropion (along with Varenicline & Nicotine replacement therapy) is a USFDA approved first-line agent for pharmacotherapy in smoking cessation.
  • Nicotine replacement therapy includes transdermal patch, gum, lozenges, oral inhaler & nasal spray.
  • Varenicline is a selective partial agonist at Alpha4-Beta2 Nicotinic A-Choline receptor, that is believed to mediate nicotine dependence.
  • Bupropion is a nicotinic receptor antagonist.
  • Bupropion/amfebutamone is used both for atypical antidepressant & smoking cessation aid.
  • Bupropion acts as a norepinephrine & dopamine reuptake inhibitor (NDRI), and alpha3 beta4-nicotinic receptor antagonist.
  • Bupropion is used in prophylaxis of nicotine addiction.
  • Bupropion/Amfebutamone decreases nicotine craving.
  • Bupropion/Amfebutamone shows increased efficacy when combined with nicotine patch.
  • Mecamylamine is a nicotine antagonist, used as an anti-smoking drug.
  • Nortryptyline is an active metabolite of amitriptyline, used as an anti-smoking drug.

 

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