آمال و طموح

Smoking Cessation كيفية التوقف عن التدخين؟

نشر في 16 يونيو 2009 في المجلس الطبّي بواسطة ONE

بسم الله الرحمن الرحيم

الاقلاع عن التدخين ليستب عمليه سهله حسب الاعتقاد السائد وكثير من المدخنين وبعد انقطاعهم عن التخدين فتره من الزمن يعودون الى السجاره , هذه العاده الخطيرة بدنيا اولا وماديا ثانيا.
في هذا المقال سوف اختصر حديثي باللغه العربيه للوصول للمفيد وبلغه مبسطه مرفقا محاضره لصيدلانيين من الولايات المتحده متخصصين بطرق التخلص من التدخين.
المقال باللغه الانجليزيه مجرد رؤوس اقلام تشمل النقاط المهمه لانواع الادويه التي تاخذ بالفم, التنشق عن طريق الانف او الفم, حقن تحت الجلد وهي معتمده لدى جمعيه الادويه والغذاء الامريكي.
يعتبر المقال باللغه الانجليزيه مرجع للاطباء والصيدلانيين لطرق معالجه المدمن على التدخين ويمكن الاطلاع عليها لمن اراد الاستفاده من المعلومات الوارده فيها.
السجاره تحتوي في مكوناتها النكوتين والقطران ومواد اخرى كما في الصورة في راس المقال وهي مواد سامه وتسبب سرطان الرئه وسرطانيات آخرى وهي المسبب الاكبر لتصلب الشرائين وامراض القلب والجلطات بانواعها وهذا الكلام تردد كثيرا بحيث الجميع يعلم مضارها تقريبا.
المدخنون انواع, منهم من يسمى المدخن البسيط وهو من يدخن عدد من السجائر يوميا وفي المناسبات ولمدد متقطعه ومنهم المدخن المدمن , وينقسم ايضا الى مدمن بعدد كميه السجائر (اكثر من 25 سجاره يوميا) ولمدد عمريه كبيرة, ولاننسى المدخنين السالبين (اي من يجالس المدخن ) وهم ايضا عرضه لنفس امراض المدخن الموجب.
ماده النكوتين شبهت مثلها كمثل المخدرات حيث انها تؤثر على خلايا خاصه في الدماغ تحفز الادمان وتساعد على زياده هرمون الدوبامين مشابه لتحفيز المخدرات.
لذا فان الطب تقدم وزادت البحوث في كيفيه التخلص من التدخين بطرق علميه تجنب عوده المدخن للسجاره.
مضار التدخين لاتقتصر على الشخص فقط وانما على من هم حوله وعلى الجنين ايضا سواء كانت الام مدخنه ام لم تكن.
وباختصار فان جمعيه الدواء والاغذيه الامريكيه اعتمدت ادويه للاطباء لمساعه المدخنين على الاقلاع وبشرط اكمال العلاج في مده 12 شهر ليتخلص المدخن نهائيا من هذه الآفه.
كثير من الناس يعتقد ان العزيمه هي العامل الوحيد للاقلاع وهذا خطأ فادح, يجوز في المدخنون الجدد او لِما تم تصنيفه سابقاً (غيرالمدمن) بالاقلاع فجائيا ولكن لاينصح بذلك.
الاقلاع عن التدخين فجأه ليس فقط يسبب عوده المدخن ولكن هناك اثار جانبيه خطيرة وهي اثار الانسحاب, منها زياده ضربات القلب واحتمال الجلطه لارتجاف القلب الشديد من الانسحاب.
طرق الاقلاع تحتاج الى فريق متخصص ومنهم الدعم النفسي وبادخال مشبهات النكوتين اما عن طريق الجلد او الفم او التنشق ولكل شخص جرعه محدده تعتمد على وزن وفتره إدمانه وليس اعتباطي كما يمارسه وللاسف من بعض الصيدلانيين في بلداننا العربيه او بترديد عباره “اسال مجرب ولاتسال طبيب” فلايقلع المدخن ابداَ.
طبعا سمعنا عن النكوتين بالعلكه او شرايط لاصقه في الجلد, اما الان فهي عن طريق الانف والرذاذ.
في بعض الاحيان نتجه لادويه خاصه بمرضى الاكتئاب وتم اكتشاف فعاليتها في الاقلاع عن التدخين.
من هذ الادويه كما في الجداول المرفقه , وايضا لكل دواء جرعات محدده وارشادات يجب على المقلع ان يسال الطبيب او الصيدلاني بكيفيه اخذها لما لها من اثار جانبيه خطيرة إن لم يتبع الارشادات وخاصه للحامل او لمرضى ياخذون أدويه آخرى مثل ادويه الاكتئاب الاخرى , فيجب ان تكون بين المتعالج والطبيب شفافيه في وجود اي دواء جانبي حتى يتفادى الاثار الخطيرة والوصول للفائدة المرجوه.
الصبر مهم حتى يقلع المدخن نهائيا وبلا رجعه , ونتمنى لكم الفائدة .

 

Pharmacotherapy for
Smoking Cessation
Venita L. Bowie, Pharm.D.
Paula Mackrides, DO

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EVIDENCE BASED
Use of smoking cessation medications as part of smoking cessation is based on solid evidence
Systemic reviews of randomized, controlled trials of smoking cessation aids, including medication, increases the chances of quitting
*****mulative data doesn’t demonstrate an advantage of one smoking cessation aid over another

So how do you select?
Patient preference
Previous patient experience
Contraindications
Patient characteristics

The Food and Drug Administration (FDA) Approved Agents
Nicotine replacement therapy (NRT) include the following forms.
Gum
Patch
Nasal spray
Inhaler
Lozenge
Oral medications

Specific RX Products
Nicoderm CQ (Transdermal)
Commit Lozenge (Nicotine Polacrilex)
Nicorette Gum (Nicotine Polacrilex)
Nicotrol Inhaler
Nicotrol Nasal Spray
Zyban (Wellbutrin)
Chantix (Varenicline)

Additional Second-line Agents
Not FDA approved
Opioids Antagonists (Naloxone, Naltrexone)
Alpha-2 adrenergic agonist (clonidine)
Tricyclic antidepressants
Nortriptyline, fluoxetine, doxepin, impiramine, paroxetine, sertraline, tryptophan, moclobenide and venlafaxine
Mecamylamine
Anxiolytics
Buspirone, doxepin, meprobamate, propranolol, oxprenolol and metoprolol
Other agents
Rimonabant (an endocannabinoid receptor antagonist)
Antibodies that bind to nicotine molecules

Pharmacotherapy for
Smoking Cessation
The Treating Tobacco Use and Dependence guideline panel recommends that all smokers (without contraindications) attempting to quit.
Pharmacotherapy needs to be offered to aid their efforts

What are the benefits of pharmacotherapy?
It increases the odds of quitting (1.5 to twofold)
Reduces the withdrawal symptoms
Some patients are provided with some “reward” produced by nicotine in the CNS

Nicotine
Nicotine is one of 2 naturally-occurring alkaloids
The second alkaloid is lobeline (less potent)
A potent ganglion and CNS stimulant
Actions are mediated via receptors specific to nicotine
Biphasic actions are dose dependent
The cortex via the locus ceruleus is where the stimulating affect occurs
The reward effects: limbic system.
Low doses = stimulating effect
High doses = reward effect

Nicotine Similarities
Nicotine is believed to be active similar to the following agents
Opioids
Cocaine
Methamphetamine
Heroin
They all share some physiologic pathways
The release of dopamine
Nicotine, like opioids, and ethanol increases the release of dopamine
Amphetamines increases the release of dopamine through displacement
Cocaine inhibits dopamine reuptake
Heroin modifies the action of dopamine in the nucleus ac*****bens and in specific areas of the brain

Nicotine
CNS stimulation
Tremors
Respiratory excitation
Convulsions (higher doses)
Respiratory failure
Other effects include
Euphoria
Psychoactive benefits (antidepressant effect)
Enhancing task performance
Addiction

Before Initiating NRT
Instructed patients to stop smoking completely as they begin nicotine cessation therapy.
If a patient is unable to quit smoking by the fourth week of therapy discontinue treatment.

Transdermal Patch
Nicoderm, Habitrol, Nicotrol, Prostep
Available dose: 11 mg up to 22 mg
Dose is dependant on cigarettes per day
Length of therapy, dosage strength and duration of wear varies by brand
Once applied, an initial increase in serum nicotine level occurs
Steady levels are maintain throughout dosing period
Patches are available in 16 and 24 hour applications
24 hour patches provide better control of cravings and withdrawal

Dose
Apply new patch every 24 hrs to non hairy, clean dry skin on the upper body or upper outer arm
> 10 cigarettes/day:
Begin with step 1 (21 mg) for 4-6 wks
Followed by step 2 (14 mg) for 2 wks
Step 3 (7 mg) for 2 wks
< 10 cigarettes/day
Begin with step 2 (14 mg) for 6 wks
Followed by step 3 (7 mg) for 2wks
Special Considerations
Patients < 100 pounds, history of cardiovascular disease
Initial dose: 14 mg/day for 4-6 wks followed by 7 mg for 2-4 weeks
Patients on > 600 mg of Cimetidine: decrease to the next lower patch size
Pregnancy Category: D
Cutting the transdermal nicotine patch in half is not recommended

Contraindications
Hypersensitivity to nicotine or components
Pregnancy
Patient’s that smoke post myocardial infarction period
Life threatening arrhythmias
Severe or worsening angina pectoris
Non smokers
Precautions
Accelerated hypertension
Allergy to adhesive tape
Cardiovascular and peripheral vascular diseases
Severe or worsening angina

Adverse Side Effects
Tachycardia
Insomnia, abnormal dreams
Pruritus, erythema
Rhinitis, cough, pharyngitis, and sinusitis
Rash
Dyspepsia, nausea, xerostomia

Drug Interactions
Cytochrome P 450 Effect:
Minor: CYP1A2, 2A6, 2C8/9, 2C19, 2D6, 2E1, 3A4
Weak inhibitor of CYP2A6, and 2E1
Cimetidine increases nicotine concentrations (gum and patch dose effected)
Monitor patients while on patch and bupropion
Nicotine increases the hemodynamic and AV blocking of adenosine
Clozapine (decreased plasma levels)
Memantine (altered plasma levels of both agents)
Niacin (increased flushing and dizziness)

Food Interactions
Lozenge: Acidic foods or beverages decrease absorption of nicotine

Commit Lozenge
(Nicotine Polacrilex)
Dosage: 2 mg and 4 mg
Patients that smoke their first cigarette within 30 minutes use 4 mg
Week 1-6: One Lozenge every 1-2 hrs
Week 7-9: One lozenge every 2-4 hrs
Weeks 10-12: One lozenge every 4-8 hrs
During the first 6 weeks use at least 9 lozenges/day
Do not use more than 1 lozenge/time
Maximum 5 Lozenges q 6hrs (20 per day)

Special Instructions
Do not eat or drink 15 minutes before use
Dissolve slowly in mouth over 20 to 30 min
Move lozenge from one side of mouth to the other until completely dissolved
Do not chew or swallow

Adverse Side Effects
Tachycardia
Headache (mild),
Nausea, vomiting indigestion, excessive salivation, belching
Mouth or throat soreness, increased appetite or hiccups
Hoarseness

Contraindications
Hypersensitivity to nicotine or components
Pregnancy category: D
Precautions
Concomitant use of other nicotine products
Concurrent medication for depression or asthma
Uncontrolled high blood pressure
History of Peptic ulcers
Recent MI, Irregular heart beats
Diabetes

Nicorette Gum
(Nicotine Polacrilex)
Dosages: 2 mg/square, and 4 mg/square
Flavors: mint, orange and original
Dose
Heavy smokers: > 25 cigarettes/day
Chew 1 piece 4 mg gum every 1-2hrs for weeks 1-6
Chew 1 piece 4 mg every 2-4 hrs for week 7-9
Chew 1 piece 4 mg every 4-8 hrs for week 10-12
Light smokers: < 25 cigarettes/day
Chew 1 piece 2 mg gum every 1-2hrs for weeks 1-6
Chew 1 piece 2 mg gum every 2-4 hrs for weeks 7-9
Chew 1 piece 2 mg every 4-8 hrs for weeks 10-12
Special Instructions
Do not eat or drink 15 minutes before using
hew gum slowly until it tingles, then park it between your cheek and gum
When tingles stops repeat process until most of it is gone (approx 30 minutes)
Wrap used pieces in paper before discarding

Adverse Side Effects
Tachycardia
Hadache (mild)
Nusea, vomiting, indigestion, excessive salivation
Jew muscle ache, hiccups, hoarseness
Dizziness, nervousness

Contraindications
Hypersensitivity to nicotine or components
Precautions
Same as the lozenge
Pregnancy Category: C
Nicotrol Inhaler
10 mg cartridge (delivers 4 mg nicotine)
1 mouthpiece, 7 storage trays (containing 6 cartridges)

Dosage
Usually 6 to 16 cartridges/day up to 12 weeks
Best effect: Inhale by continuous puffing (20 minutes)
Wean gradually over 6 to 12 weeks
Duration of treatment 3 months

Special Considerations
Separate mouthpiece, remove and discard used cartridge;
Clean mouthpiece with soap and water and store in plastic case

Adverse Side Effects
Throat and mouth irritation
Dizziness

Nicotrol Nasal Inhaler
Dosage: 10 mg/ml delivers 0.5 mg/spray
2 sprays (1 in each nostril) 1 to 2 times/hr
Max doses: 5 doses per hour
Max 40 doses in a 24 hour period
Maximum duration: 3 months

Special Considerations
Patients should be instructed not to sniff, swallow, or inhale through the nose as the spray is being administered.
Advised to administer the spray with the head tilted back slightly.
Zyban (Bupropion)
An antidepressant that is different in structure from tricyclic, (SSRI), and MAOI.
The mechanism of action as an aid to smoking cessation is unknown
Relatively weak inhibitor of the neuronal uptake of serotonin, NE, and dopamine.
The primary MOA is thought to be dopaminergic and or noradrenergic

Dose: Smoking Cessation
Initiate 150 mg once daily for 3 days
Increase to 150 mg BID
Initial response: 1 to 2 weeks
Treatment for 7- 12 weeks
Combination treatment of bupropion sustained release and a nicotine transdermal system may be prescribed
Pharmacokinetics
Rapidly absorbed
Protein binding 84% (sustained and immediate release)
Liver major site of metabolism
Activity of the metabolites ranges from 20% to 50% potency of parent compound
Renally excreted
Elimination of the active metabolite may be reduced in pts with renal impairment

Drug Interactions
Concomitant administration of bupropion and agents that lower seizure threshold should be used with caution
Betamethasone, Budesonide, Danazol, and Dexamethasone (not a complete list)
Increase risk of serotonin syndrome with Zyvox (linezolid)
Drug Interactions
Cytochrome P450 substrate effect
Weak inhibitor of: CYP2D6 (however can effect serum levels of some agents)
Minor for: CYP1A2, 2A6, 2C8/9, 2E1, and 3A4
Major for : 2B6

Black Box WARNING
Black box warning pertains to treating patients with depression
Antidepressants increased the risk of suicidal thinking and behavior (suicidality) in short-term studies in children and adolescents with Major Depressive Disorder (MDD) and other psychiatric disorders.
Contraindications
Seizure disorders
Patients undergoing abrupt discontinuation of alcohol or sedatives
Prior or current diagnosis of bulimia or anorexia
Concomitant MAO inhibitor
Hypersensitivity to bupropion products

Precautions
Pregnancy Category: C
Addiction to opiates, cocaine, or stimulants
Diabetes treated with oral hypoglycemics or insulin
Hypertension, myocardial infarction, or unstable heart disease
Medications or treatments that lower the seizure threshold

Adverse Side Effects
Dizziness
Headache
Insomnia
Nausea, Xerostomia
Pharyngitis
Agitation

Patient Information
Bupropion can provide beneficial effects with smoking cessation
Must be taken on a regularly scheduled basis
Behavior and lifestyle modifications must be combined

Chantix (Varenicline)
Newest agent for smoking cessation
Two strengths: 0.5 mg and 1 mg
Approved by FDA 5/10/2006
A partial agonist selective for alpha-4-beta-2 nicotinic acetylcholine receptor

Mechanism of Action
Varenicline binds with high affinity and selectivity at the alpha-4-beta-2 neuronal nicotinic acetylcholine receptors
Efficacy of varenicline is believe to be at the sub-type of the nicotinic receptor
Binding produces its agonist activity
Nicotine is prevented from binding to the alpha-4-beta-2 receptors
Stimulation of the central nervous mesolimbic can not occur
Reinforcement and reward can not occur

Pharmacokinetics
Peak plasma concentration: 3-4hrs
Steady state reached in 4 days (following multiple dosing)
Half-life: parent compound 24 hours
Protein binding: 20% or less
Liver metabolism: minimum
92% of the drug is excreted in the urine

Contraindications
Hypersensitivity to varenicline tartrate or any component of the formulation
Other specific contraindications have not been determined

Precautions
Use caution in renal dysfunction (dose adjustment required)
Altered pharmacokinetics or pharmacodynamics of some drugs including theophylline, warfarin and insulin may occur with smoking cessation
Dose reduction should be considered with intolerable nausea

Dose
Recommended starting dose:
1-week titration: 0.5 mg orally once daily on days 1 thru 3, then 0.5 mg twice daily on days 4 thru 7.
Then 1 mg twice daily for 12 weeks (including 1 week titration).
1 mg BID is the recommended dose

Dosage Adjustment for
Renal Impairment
Mild to moderate renal impairment, no dosage adjustment is required
For severe renal impairment (CrCl < 30 ml/min)
Recommended starting dose is 0.5 milligrams (mg) orally once daily
Patients may be titrated up to 0.5 mg twice daily

Special Instructions
Therapy should begin 1 week prior to the date set by patients to stop smoking
Patients that are sensitive to varenicline adverse effects (nausea, headache, insomnia), the dose may be lowered
Educational materials and counseling on smoking cessation should also be provided.
Efficacy after 12 months

Adverse Side Effects
Rash
Abdominal pain, flatulence, and constipation
Nausea (up to 40%), Indigestion, altered taste and increase appetite
Headache, abnormal dreams and insomnia

Contraindications
Hypersensitivity to varenicline or any component of the formulation
Precautions
Renal dysfunction
During smoking cessation the pharmacokinetics or pharmacodynamics of some drugs including theophylline, warfarin and insulin may be altered
Pregnancy Category: C

Brief Overview Treatment Duration
Zyban: 7 to 12 weeks
Nicotine gum: Up to 12 weeks
Nicotine Inhaler: Up to 6 months
Nicotine nasal inhaler: 3 to 6 months
Nicotine patch: 8 weeks (4 wks, then 2 wks, then 2 wks)

FDA Approved Agents
Efficacy at 12 months
Nicotine patch: 11.1% vs. 5.2 placebo
Nicotine nasal spray: no current data
Nicotine inhaler: 16.9% vs. 9.1%
Nicotine gum: 27.3% vs. 16.5%
Bupropion (Zyban): 18.5% vs. 6.6%

Efficacy at 12 months with NRT plus Behavioral Intervention
Nicotine patch
Placebo 5.2%
With intervention 11.1%
Nicotine gum
Placebo 16.5%
With intervention 27.3%
Nicotine inhaler
Placebo 9.1%
With intervention 16.9%
Bupropion
Placebo 13.9%
With intervention 20.0%
Combination Therapy:
Studies have shown smokers who use combination products greatly increases their chances of remaining smoke-free

Summary: Nicotine replacement therapy + behavior therapy increases chances of quitting Combination therapy greatly increases success rates.
click on the figure to enlarge

ملحوظة: الاخت سحر العيون:النكوتين ماده مدمنه صحيح ولكن فقط للعلاج حتى يتم الانقطاع عنها وحسب مقالي السابق فان السجاره لاتحتوي على النكوتين فقط وانما مواد سامه اخرى. النكوتين يمنع لمايسمى “النهم”craving لادمان النكوتين. شكرا على المرور والتعليق وهذا موقع لكي وللقراء للاستفاده وفهم النهم لماده النكوتين

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