Tag: Anti-Smoking Drugs

Anti-Smoking Drugs

ANTI-SMOKING DRUGS

Q. 1

Nicotine replacemen therapy is available in all forms except –

 A

Chewing gum

 B

Lozenges

 C

Patch

 D

Tablets

Q. 1

Nicotine replacemen therapy is available in all forms except –

 A

Chewing gum

 B

Lozenges

 C

Patch

 D

Tablets

Ans. D

Explanation:

Ans. is ‘d’ i.e., Tablets

o Nicotine replacement is available as nicotine patch (most commonly used), chewing gum, nasal sprays, inhalers and lozenges.


Q. 2

Which of the following drugs, is used for Smoking Cessation?

 A

Naltrexone

 B

Bupropion

 C

Buprenorphine

 D

Methadone

Q. 2

Which of the following drugs, is used for Smoking Cessation?

 A

Naltrexone

 B

Bupropion

 C

Buprenorphine

 D

Methadone

Ans. B

Explanation:

Answer is B (Bupropion):

Bupropion (along with Varenicline and Nicotine replacement therapy) is a USFDA approved first line agent for pharmacotherapy in Smoking Cessation.

USFDA Approved Agents for Smoking Cessation

  • Nicotine Replacement Therapy (Transdermal Patch, gum, lozenges, oral inhaler, nasal spray)
  • Bupropion (Atypical Antidepressant with dopaminergic and noradrenergic activity)
  • Varenicline (Selective partial agonist at the Alpha4-Beta2 Nicotinic A-Choline receptor that is believed to mediate nicotine dependence)

Clonidine and Nortriptyline are two other medications that have efficacy but are NOT USFDA approved for this indication. These are classified as second line agents.


Q. 3

True regarding bupropion is:     

September 2009

 A

Dopamine reuptake stimulator

 B

It is an antianxiety drug

 C

No precipitation of seizures

 D

Nicotinic receptor antagonist

Q. 3

True regarding bupropion is:     

September 2009

 A

Dopamine reuptake stimulator

 B

It is an antianxiety drug

 C

No precipitation of seizures

 D

Nicotinic receptor antagonist

Ans. D

Explanation:

Ans. D: Nicotinic receptor antagonist

Bupropion/amfebutamone is an atypical antidepressant and smoking cessation aid.

It acts as a norepinephrine and dopamine reuptake inhibitor (NDRI), as well as alpha3 beta4-nicotinic receptor antagonist.

Bupropion belongs to the chemical class of aminoketones and is similar in structure to stimulants cathinone and diethylpropion, and to phenethylamines in general.

Bupropion is an effective antidepressant on its own but it is particularly popular as an add-on medication in the cases of incomplete response to the first-line selective serotonin reuptake inhibitor (SSRI) antidepressant.

Since it does not inhibit serotonin reuptake at all (or very insignificantly), bupropion does not cause weight gain or sexual dysfunction like the SSRI group of antidepressants.

It precipitates seizures

Quiz In Between


Q. 4

Drug used in the prophylaxis of nicotine addiction:

NIMHANS 08; Manipal 09; Maharashtra 10, WB 11

 A

Diazepam

 B

Naloxone

 C

Bupropion

 D

Acamprosate

Q. 4

Drug used in the prophylaxis of nicotine addiction:

NIMHANS 08; Manipal 09; Maharashtra 10, WB 11

 A

Diazepam

 B

Naloxone

 C

Bupropion

 D

Acamprosate

Ans. C

Explanation:

Ans. Bupropion


Q. 5

All are used in nicotine de-addiction, except:

NIMHANS 10, 11

 A

Bupropion

 B

Clonidine

 C

Nicotine gum

 D

Buspirone

Q. 5

All are used in nicotine de-addiction, except:

NIMHANS 10, 11

 A

Bupropion

 B

Clonidine

 C

Nicotine gum

 D

Buspirone

Ans. D

Explanation:

Ans. Buspirone


Q. 6

Varenicline acts by ‑

 A

Partial nicotine receptor agonist

 B

Nicotine receptor antagonist

 C

Both agonist and antagonist at nicotine receptor

 D

None of the above

Q. 6

Varenicline acts by ‑

 A

Partial nicotine receptor agonist

 B

Nicotine receptor antagonist

 C

Both agonist and antagonist at nicotine receptor

 D

None of the above

Ans. A

Explanation:

Ans. is ‘a’ i.e., Partial nicotine receptor agonist

Varenicline

  • It is partial agonist at the nicotine receptor.
  • It is used in nicotine addicts.

Quiz In Between



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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