Smoking Cessation: Pharmacotherapy

Pharmacy and Therapeutics

First line agents

  1. Nicotine replacement therapy (NRT): Nicotine gum, transdermal patch, lozenges, nasal spray, inhaler.
  2. Varenicline (Chantix)
  3. Bupropion

Second line agents 
For people who can’t use a first-line agent or need an adjunct with it.

  1. Nortriptyline
  2. Cytisine (not available in the U.S.) – is a partial agonist at the alpha-4 beta-2 nicotinic acetylcholine receptor  (like varenicline)

Combination therapies (more effective than single)
If a patient has no response to the initial agent, switched to a different medication. If that doesn’t work, use combination therapies.

  1.  Combination of two NRT products (a patch plus a short-acting form such as the gum or lozenge) – Combination of two NRT may be used as first-line agent.
  2.  Nicotine patch + Varenicline (source: Uptodate.com)
  3. Bupropion + Varenicline,
  4. Bupropion + NRT,
  5. Nortriptyline + NRT.

Arch Intern Med. 2004 Nov 8;164(20):2229-33.
JAMA. 2016 Jan 26;315(4):371-9. 

Medications Approved by the U.S. Food and Drug Administration (FDA) for Smoking Cessation:

Medication Prescribing info Mechanism of Action / Side Effects / Comments
Nicotine gum (Nicorette gum) -Comes as 2mg or 4mg per gum.
1st cigarette >30min after waking
Dose: 2 mg PO q1-2h x6wk, then q2-4h x3wk, then q4-8h x3wk; Start: on cigarette quit day; Max: 24 pieces/24h; Info: use >9 pieces/day during initial 6wk; avoid food/drink 15min before and after use
1st cigarette <30min after waking
Dose: 4 mg PO q1-2h x6wk, then q2-4h x3wk, then q4-8h x3wk; Start: on cigarette quit day; Max: 24 pieces/24h; Info: use >9 pieces/day during initial 6wk; avoid food/drink 15min before and after use		 Nicorette Gum = (Nicotine Transmucosal)
(May be used by gradual quitters while reducing the number of cigarettes they are smoking).
Nicotine lozenge
Nicotine transdermal patch -Start high and then taper down.
-Stop cigarette use at tx onset.
6-10 Cigarette/day smoker:
-Apply 14mg patch qd x 6 wk, then apply 7 mg patch qd x 2 wk.
> 10 Cigarette / day smoker:
Apply 21 mg patch qd x 6wk, then apply 14mg patch qd x 2wk, then apply 7mg patch qd x 2wk.
Nicotine Nasal Spray
Nicotine inhaler
Bupropion ER -Bupropion ER  150 mg ER po BID x 7-12 wk
-Start dose 150 mg ER po qd x 3 days;  Max: 300 mg / day ER.
-Separate doses by at least 8 hours;
-Last dose no later than 6 pm;
-Stop smoking after 5-7 days of tx; do not cut/crush/chew ER tab.		 MOA: Inhibits neuronal uptake of NE and DA.
-Don’t give it to pts with seizures or low seizure threshold.
Varenicline A) 28-day starting convenience pack has 0.5mg tab x11 and 1 mg tab x42.

Rx: Start 0.5 mg PO qd x 3 days, then 0.5 mg PO bid x 4 days, then 1 mg PO bid x 21 days.

B) 28-day continuing convenience pack contains 1 mg tab x56.
Rx: Take 1mg PO bid for 28 days.

**Take with food. Start drug 1wk before quit date if quit date planned; stop smoking 8-35 days after starting drug if quit date unplanned.

**Initial tx=12wk (1 starting pack + 2 continuing packs); may continue additional 12wk if initial tx successful.

 

 MOA: Agonizes and blocks alpha-4-beta-2 nicotinic acetylcholine receptors.

Bupropion = Wellbutrin; NE = Norepinephrine; DA = Dopamine. Varenicline = Chantix

Nortriptyline  (like Bupropion) is another antidepressant that has been showed to help with tobacco cessation. SSRI’s don’t work. Use Nortriptyline in patients who can’t use Varenicline (Chantix) or Bupropion and Nicotine replacement isn’t working.

**Bupropion can cause weight loss.
Nortriptyline can cause weight gain. So does Amitriptyline.

Nicorette (Nicotine gum) manufacturer’s FAQs.

Any of the above medications work just as well. The choice of medication is usually based on the patient’s preferences and risks. E.g. Bupropion can’t be taken by patients who have hx of seizures in self or family.

On one patient, Dr. T did:
First: He tried the patch.
-Nicotine 14mg/24hr daily transdermal patch. Apply 1 patch by transdermal route every day.
When it didn’t work, he d/c that and started both Wellbutrin and nicotine gum.

-1) Wellbutrin SR 150mg. Take 1 tablet po QD for 3 days, then increase to one tablet po BID. He tries Wellbutrin for three months to help them quit. If they don’t, quit, he d/c’s med.
-2) Nicotine (Polacrilex) 4mg gum. Chew one piece of gum by oral route every 2hrs as needed and as directed.

The pt quit and just continued to take only the nicotine gum for his cravings.

References and Resources

JAMA. 2016 Jan 26;315(4):371-9. Effects of Nicotine Patch vs Varenicline vs Combination Nicotine Replacement Therapy on Smoking Cessation at 26 Weeks: A Randomized Clinical Trial. https://www.ncbi.nlm.nih.gov/pubmed?term=26813210

Arch Intern Med. 2004 Nov 8;164(20):2229-33.  A randomized trial of nortriptyline combined with transdermal nicotine for smoking cessation. https://www.ncbi.nlm.nih.gov/pubmed?term=15534159

Click to access practice-manual.pdf

http://www.cdc.gov/tobacco/

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