NICOTINE IS AN ADDICTIVE SUBSTANCE

Image 1: Nicotine.

Nicotine is an alkaloid found in the nightshade family of plants (Solanaceae), predominantly in tobacco. In low concentrations (an average cigarette yields about 1 mg of absorbed nicotine), the substance acts as a stimulant in mammals and is one of the main factors responsible for the dependence-forming properties of tobacco smoking.

It is highly addictive – as addictive as heroin or cocaine. Over time, the body becomes both physically and psychologically dependent on nicotine. Studies have shown that smokers must overcome both of these addictions to be successful at quitting and staying quit.

ACTION

When tobacco is smoked, nicotine is absorbed by the lungs and quickly moved into the bloodstream, where it is circulated throughout the brain. This happens rapidly, nicotine reaches the brain within 8 seconds after the inhalation. Nicotine can also enter the bloodstream through the mucous membranes that line the mouth (if tobacco is chewed) or nose (if snuff is used), and even through the skin.

The nicotine molecule is shaped like a neurotransmitter called acetylcholine. Acetylcholine and its receptors are involved in many functions, including muscle movement, breathing, heart rate, learning, and memory. They also cause the release of other neurotransmitters and hormones that affect your mood, appetite, memory, and more. When nicotine gets into the brain, it attaches to acetylcholine receptors and mimics the actions of acetylcholine.

Nicotine also activates areas of the brain that are involved in producing feelings of pleasure and reward. Nicotine also raises the levels of a neurotransmitter called dopamine in the parts of the brain that produce feelings of pleasure and reward. Dopamine, which is sometimes called the pleasure molecule, is the same neurotransmitter that is involved in addictions to other drugs such as cocaine and heroin.

Nicotine at first causes a release of glucose from the liver and adrenaline from the adrenal medulla, this causes stimulation, feelings of relaxation, calmness, alertness and even a mildly euphoric state. By reducing the appetite and raising the metabolism, some smokers may lose weight as a consequence. It allows the mouth to be stimulated without food and the taste of tobacco smoke may reduce the appetite. Nicotine enhances concentration, learning, and memory due to the increase of acetylcholine. It also enhances alertness due to the increases of acetylcholine and norepinephrine. Arousal is increased by the increase of norepinephrine. Pain is reduced by the increases of acetylcholine and beta-endorphin. Anxiety is reduced by the increase of beta-endorphin.

The effects of nicotine last from five minutes to two hours. Mostly cigarettes contain 0.1 to 2.8 milligrams of nicotine. When smokers wish to achieve a stimulating effect, they take short quick puffs, which produces a low level of blood nicotine and stimulates nerve transmission. If one wishes to relax, deep puffs are needed to produce a high level of blood nicotine, which depresses the passage of nerve impulses, producing a mild sedative effect. At low doses nicotine potently enhances the actions of norepinephrine and dopamine in the brain causing a drug effect typical of pyschostimulants. At higher doses nicotine enhances the effect of serotonin and opiate activity, producing a calming, pain killing effect. Nicotine is unique in comparison to most drugs, as its profile changes from stimulant to sedative/pain killer in increasing dosages and use.

Nicotine’s addictive nature has been found to activate reward pathways—the circuitry within the brain that regulates feelings of pleasure and euphoria. Dopamine is one of the key neurotransmitters actively involved in the brain. By increasing the levels of dopamine within the reward circuits in the brain, nicotine acts as a chemical with intense addictive qualities. In many studies it has been shown to be more addictive than cocaine and heroin, though chronic treatment has an opposite effect on reward thresholds. Nicotine causes down-regulation of the production of dopamine and other stimulatory neurotransmitters as the brain attempts to compensate for artificial stimulation. In addition, the sensitivity of nicotinic acetylcholine receptors decreases. To compensate for this compensatory mechanism, the brain in turn upregulates the number of receptors, convoluting its regulatory effects with compensatory mechanisms meant to counteract other compensatory mechanisms. The net effect is an increase in reward pathway sensitivity, opposite of other drugs of abuse (namely cocaine and heroin, which reduces reward pathway sensitivity). This neuronal brain alteration persists for months after administration ceases. Due to an increase in reward pathway sensitivity, nicotine withdrawal is relatively mild compared to ethanol or heroin withdrawal.

There is only anecdotal evidence about abuse or addiction with nicotine gum or nicotine patches due to its stimulation of the nicotinic receptors (mimicking the effects of acetylcholine) it has been reported as a useful tool for the induction of lucid dreams, where a nicotine patch is applied after 4-6 hours of normal sleep and the subject falls back to sleep (into a more REM intense sleep cycle). Non-lucid dreams may become vivid, more memorable and some report a higher frequency of disturbing dreams. However it should be stressed that a consistent use of nicotine will desensitize the nicotinic receptors and therefore addicts are actually far less likely to achieve lucid dreams.

THE REASON FOR QUITTING

As well as causing health problems in the smokers themselves, cigarette smoke in the air can also affect other people. Smoking causes about 30 % of all cancer deaths, 17 % of all heart disease deaths and at least 80 % of deaths from bronchitis and emphysema. Smoking while pregnant leads to an increased risk of miscarriage, bleeding during pregnancy, premature birth, low birth-weight babies and Sudden Infant Death Syndrome.

Smoking effects include:

• Premature wrinkling of the skin
• Bad breath
• Stained teeth
• Gum disease
• Bad smelling clothes and hair
• Yellow fingernails

Quitting the tobacco habit offers immediate benefits and some that will develop gradually over time. These rewards can improve day-to-day life immensely.

• Food tastes better.
• Your sense of smell returns to normal
• Ordinary activities no longer leave you out of breath (for example, climbing stairs or light housework)

WHAT ARE THE BENEFITS OVER TIME?

• 20 minutes after quitting: Heart rate and blood pressure drops
• 12 hours after quitting: The carbon monoxide level in your blood drops to normal
• 2 weeks to 3 months after quitting: Circulation improves and your lung function increases
• 1 to 9 months after quitting: Coughing and shortness of breath decrease; cilia (tiny hair-like structures that move mucus out of the lungs) regain normal function in the lungs, increasing the ability to handle mucus, clean the lungs, and reduce the risk of infection
• 1 year after quitting: The excess risk of coronary heart disease is half that of a smoker's
• 5 years after quitting: Stroke risk is reduced to that of a nonsmoker 5 to 15 years after quitting
• 10 years after quitting: The lung cancer death rate is about half that of a continuing smoker's. The risk of cancer of the mouth, throat, esophagus, bladder, cervix, and pancreas decrease
• 15 years after quitting: The risk of coronary heart disease is that of a nonsmoker's

Expenses

The prospect of better health is a major reason for quitting, but there are others as well. Smoking is expensive. It is not hard to calculate how much you spend on smoking. And this does not include other possible expenses, such as higher costs for health and life insurance, as well as the health care costs due to tobacco-related conditions.

Social Acceptance

Smoking is less socially acceptable now than it was in the past. Most workplaces nowadays have some type of smoking restrictions. Some employers even prefer to hire nonsmokers.

Employees who are ill more often than others can raise an employer’s need for expensive temporary replacement workers. They can increase insurance costs both for other employees and for the employer, who typically pays part of the workers’ insurance premiums. Smokers in a building also typically increase the maintenance costs of keeping odours at an acceptable level, since residue from cigarette smoke clings to carpets, drapes, and other fabrics.

Landlords may choose not to rent to smokers since maintenance costs and insurance rates may rise when smokers occupy buildings.

Friends may ask smokers not to smoke in their houses or cars. Public buildings, concerts, and even sporting events are largely smoke-free. And more and more communities are restricting smoking in all public places, including restaurants and bars. Like it or not, finding a place to smoke can be a hassle.

Smokers may find their opportunities for dating or romantic involvement, including marriage, are largely limited to other smokers, who make up only about 1/4th of the population.

Health of Others

Smoking not only harms the health of those who smoke but also the health of those around them. Exposure to second-hand smoke, also called environmental tobacco smoke or passive smoking, includes exhaled smoke as well as smoke from burning cigarettes.

Second-hand smoke causes thousands of deaths each year from lung cancer and heart disease in healthy non-smokers.

Smoking by mothers is linked to a higher risk of their babies developing asthma in childhood, especially if the mother smokes while pregnant. It is also associated with sudden infant death syndrome (SIDS) and low-birth weight infants. Babies and children raised in a household where there is smoking have more ear infections, colds, bronchitis, and other respiratory problems than children from non-smoking families. Second-hand smoke can also cause eye irritation, headaches, nausea, and dizziness.

NICOTINE WITHDRAWAL

The absence of nicotine leads to withdrawal symptoms, physical and mental. Physically, the body reacts to the absence of nicotine. Psychologically, the smoker is faced with giving up a habit, which requires a major change in behaviour. Both must be addressed in order for the quitting process to work.

Withdrawal symptoms can include:

• dizziness (which may only last 1-2 days in the beginning)
• depression
• feelings of frustration and anger
• irritability
• sleep disturbances, including having trouble falling asleep, staying asleep and having bad dreams or even nightmares
• trouble concentrating
• restlessness
• headache
• tiredness
• increased appetite

These symptoms can lead the smoker to again start smoking cigarettes again to boost blood levels of nicotine back to a level where there are no symptoms.

METHODS OF QUITTING

Quitting “cold turkey”

The most popular and well-known way smokers choose to quit smoking is what is known as "cold turkey." The phrase cold turkey is understood to mean to quit smoking abruptly, often without forethought or preparation, nor a gradual reduction in amount smoked. Most people also assume cold turkey means to quit smoking without using any smoking cessation aids such as nicotine gum or patches.

The origins of the phrase cold turkey are not completely clear but some quick searches online reveal several explanations. Origin of the phrase; cold turkey is the state of drug withdrawal when the addicts blood is directed to the internal organs leaving the skin white and with goose bumps and thus resembling a turkey.

Whatever the actual origin, quitting smoking cold turkey is probably the most popular, while not necessarily the most successful, method for quitting. It may also be the most challenging due to the severity of withdrawal symptoms the new ex-smoker faces.

One can improve chances for permanently quitting with the cold turkey method if he/she follows a few guidelines:

• Understand that withdrawal symptoms such as irritability, tiredness and more, may be fairly intense, but they will lessen after just a few days.
• Drink lots of water to help your body flush itself out quickly.
• Keep a straw or other cigarette substitute handy to keep your hands and mouth busy.
• When cravings hit, close your eyes and count down from 10 to 0, very slowly. Breathe deeply with each count.
• Call a friend when you feel like reaching for a smoke. Divert your attention.
• Take a quick walk, even if it is just to the bathroom or mailbox.

Strong willpower is often associated with using cold turkey to quit smoking. While having strong willpower is important, success ultimately depends on how badly one wants to quit and whether or not they believe they can do it. If you want to quit more than you want to smoke, and you believe that you can quit, you'll likely be successful.

Smoking cessation support and counselling

Smoking cessation support and counselling groups offer group or individual therapy which can help people who want to quit. Some programs employ a combination of coaching, motivational interviewing, cognitive behavioural therapy, and pharmacological counselling.

Telephone counselling is more convenient for many people than some other support programs. It does not require transportation or childcare, it is available nights and weekends. Counsellors may recommend a combination of methods including medicines, local classes, self-help brochures, and/or a network of family and friends.

These specialists help plan a quit method that fits each person's unique smoking pattern. People who use telephone counselling stop smoking at twice the rate of those who don't get this type of help. With guidance from a counsellor, quitters can avoid common mistakes that may self-destruct a quit attempt.

The service, provided by National smokers quitline (Ireland) can be accessed every day from 8am to 10pm. Smokers who ring the Call save number 1850 201 203 (or 0800 169 0 169 in the UK for NHS Smoking Helpline) will have the option of:

• Availing of on line counselling by trained staff.
• Being referred for professional help in their own local area, or
• Simply having an information pack sent to them by post.

Support of Family, Friends, and Quit Programs

Many former smokers say a support network of family and friends was very important during their quit attempt. Other people who may offer support and encouragement are co-workers, your family doctor, and members of support groups for quitters. You can check with your employer, health insurance company, or local hospital to find support groups or visit the website of ASH Ireland (Action on smoking and health) – www.ash.ie.

ASH Ireland is focused on reducing the impact of tobacco use in Irish society. The organization uses its independence to focus on “the issue” and ensures it is never compromised.

If you are thinking of stopping smoking you can also contact The National Quitline at 1850 201 203 or your local health board on 274 4297 or The Irish Heart Foundation, 4 Clyde Road, Ballsbridge, Dublin 4 on 01 668 50 01.

Important things when looking for a Stop-Smoking Program

Stop smoking programs are designed to help smokers recognize and cope with problems that come up during quitting and to provide support and encouragement in staying quit. The best programs will include either individual or group counseling. There is a strong association between the intensity of counseling and the success rate. In general, the more intense the program, the greater the likelihood of success.

For example, intensity may be increased by having more or longer sessions or by increasing the number of weeks over which the sessions are given. So, when considering a program, look for one that has the following:

• Session length – at least 20 to 30 minutes per session
• Number of sessions – at least 4 to 7 sessions
• Number of weeks – at least 2 weeks

Be certain the leader of the group has training in smoking cessation. Some communities have a Nicotine Anonymous group that holds regular meetings. This group applies the principles of Alcoholics Anonymous to the addiction of smoking. This may include admitting you are powerless over your addiction to nicotine and having a sponsor to talk with when you are tempted to smoke. There is no fee for this program.

There are some programs to watch out for as well, all programs are ethical. You should be concerned about programs that do the following:

• Promise instant, easy success with no effort on your part.
• Use injections or pills, especially "secret" ingredients (nicotine replacement is covered elsewhere).
• Charge a very high fee.
• Are not willing to provide references from people who have taken the class.

Nicotine replacement therapy - NRT

The aim of the therapy is to assist smoking cessation by providing a constant level of nicotine above that which is associated with withdrawal. No form of NRT can replicate the rapid nicotine delivery from a cigarette. Researches have shown that when a smoker uses NRT to help them quit, they have a better chance of being successful compared to those who try to do it by on willpower alone.

Nicotine levels in the body delivered by NRT products range between one-third and two-thirds of that derived from cigarette smoke. The smoker can then gradually wean themselves off the nicotine once their smoking behaviour has been changed.

Evidence show that NRT is also safe in patients with stable cardiac disease such as angina pectoris. Evidence is lacking in acutely unstable patients, but NRT would produce lower peak and cumulative nicotine exposure levels than smoking, without delivering the increased carboxyhaemoglobin and the many other vasoactive compounds in smoke.

Nicotine transdermal patches

Nicotine transdermal patches are designed to release nicotine slowly. Immediately after application, there may be relatively rapid transfer of nicotine from the adhesive layer. In steady-state phase, nicotine will exist in the patch, in a skin "reservoir" and in the circulation. The presence of the skin reservoir reduces the rate of decay of plasma levels after the patch is removed. Patches come in a variety of dose strengths from 7 mg to 21 mg, and in preparations designed to be used for 16 or 24 hours.

Application: each morning on a rotational basis to a variety of non-hairy skin sites. The 16 hour preparations are useful for smokers who experience insomnia or other nocturnal symptoms.
Local skin reactions are the commonest adverse effect. This can be minimized by rotation among a number of sites of application, but can be severe enough to require discontinuation.

Patches provide a measured dose of nicotine through the skin. As the nicotine doses are lowered by switching patches over a course of weeks, the tobacco user is weaned off nicotine. Several types and different strengths are available. Package inserts describe how to use the product as well as special considerations and possible side effects.

• The 16-hour patch works well for light-to-average tobacco users. It is less likely to cause side effects like skin irritation, racing heartbeat, sleep problems, and headache. But it does not deliver nicotine during the night, so it is not helpful for early morning withdrawal symptoms.
• The 24-hour patch provides a steady dose of nicotine, avoiding peaks and troughs. It helps with early morning withdrawal. However, there may be more side effects such as disrupted sleep patterns and skin irritation.

Depending on body size, most tobacco users should start using a full-strength patch (15-21 mg of nicotine) daily for 4 weeks, and then use a weaker patch (5-14 mg of nicotine) for another 4 weeks. The patch should be applied in the morning to a clean, dry area of the skin without much hair. It should be placed below the neck and above the waist - for example, on the arm.

Side effects are related to:

• The dose of nicotine
• The brand of patch
• Individual skin characteristics (such as the person’s tendency to have a skin reaction to the patch)
• How long you use the patch
• How it is applied

Some possible side effects of the nicotine patch include:

• Skin irritation – redness and itching
• Dizziness
• Racing heartbeat
• Sleep problems or unusual dreams
• Headache
• Nausea
• Vomiting
• Muscle aches and stiffness

What to do about side effects:

• Try a different brand of patch if skin irritation occurs.
• Reduce the amount of nicotine by using a lower dose patch.
• Sleep problems may be temporary and pass within 3 or 4 days. If not (and you're using a 24-hour patch), try switching to a 16-hour patch.
• Stop using the patch and try a different form of nicotine replacement.

Patches can be purchased both with and without a prescription and some NRT products are also available free of charge to eligible persons on the medical card.

Acute dosing forms

Benefit of acute dosing products is that both the amount and timing of doses can be titrated by the user. Control over the timing of self dosing is also key, because it enables smokers to use NRT medications when they encounter particularly strong cravings or threats to abstinence. This dosing forms of use requires some explanation.

Abstinence from tobacco causes tonic disruptions of function, including rises in overall levels of craving. This background level of craving is punctuated, however, by acute episodes of more intense craving. These episodes are typically provoked by situational stimuli, such as seeing someone smoke, the ringing of the telephone, or experiencing emotional upset. Notably, nicotine patches do not provide the means to immediately respond to breakthrough cravings.

Gum

Gums contain nicotine (2 mg or 4 mg per piece) in a resin base. The gum should be chewed slowly and then left between the cheek and gum. Over the next 20 – 30 minutes, the gum should be chewed intermittently and repositioned. Because nicotine is poorly absorbed in an acid environment, acid drinks such as fruit juices should be avoided. It is preferable for patients to use gum on a regular basis. While extra doses may not rapidly increase nicotine levels, the process of their use is a ritual that is in some ways analogous to smoking, and this may be an advantage.

If one smokes a pack or more per day, smokes within 30 minutes of rising, or has trouble not smoking in restricted areas, they may need to start with the higher dose (4 mg). No more than 20 pieces should be used in one day. Nicotine gum is usually recommended for 1 to 3 months, with the maximum being 6 months. Tapering the amount of gum chewed may help to stop using it.

If one has sensitive skin, they may prefer the gum to the patch. Another advantage of nicotine gum is that it allows the control of nicotine doses. The gum can be chewed as needed or on a fixed schedule during the day. The most recent data have shown that scheduled dosing is more effective. A schedule of 1 to 2 pieces per hour is common. On the other hand, with an as-needed schedule, you can chew more gum during a craving.

Some possible side effects of the gum:

• Bad taste
• Throat irritation
• Mouth sores
• Hiccups
• Nausea
• Jaw discomfort
• Racing heartbeat

Symptoms related to the stomach and jaw are usually caused by improper use of the gum, such as swallowing nicotine or chewing too rapidly. The gum can also cause damage to dentures and dental prostheses.

Long-term dependence is one possible disadvantage of nicotine gum. 15% to 20% of gum users who successfully quit smoking continue using the gum for a year or longer. Although the maximum recommended length of use is 6 months, continuing to use the gum is likely to be safer than going back to smoking. But since there is little research on the health effects of long-term nicotine gum use, most health care providers still recommend limiting its use to 6 months.

Nicotine nasal spray

This type of dosage form delivers nicotine quickly to the bloodstream as it is absorbed through the nose. It is however not available in Ireland at present. Where available it is available only by prescription.
The nasal spray immediately relieves withdrawal symptoms and offers a sense of control over nicotine cravings. Because it is easy to use, smokers report great satisfaction. However, since this product contains nicotine, it can be addictive. It is recommended the spray be prescribed for 3 month periods and should not be used for longer than 6 months.

The device is a multidose bottle with a pump that delivers 0.5 milligram of nicotine per 50 microliter squirt. Each dose consists of two squirts, one for each nostril. Nicotine is absorbed into the blood rapidly relative to all other NRT forms. Time to peak plasma concentration with nasal administration is around 11 to 13 minutes for 1 mg doses.

The most common side effects last about 1 to 2 weeks and can include the following:

• Nasal irritation
• Runny nose
• Watery eyes
• Sneezing
• Throat irritation
• Coughing

There is also the danger of using more than is needed. If one has asthma, allergies, nasal polyps, or sinus problems, the doctor may suggest another form of nicotine replacement.

Nicotine inhalers

Nicotine inhalers were introduced in 1998 and consist of a plastic tube with a nicotine cartridge inside. When one puffs on the inhaler, the cartridge provides a nicotine vapour. Unlike other inhalers, which deliver most of the medication to the lungs, the nicotine inhaler delivers most of the nicotine vapour to the mouth. In terms of similar behaviour, nicotine inhalers are the closest thing to smoking a cigarette, which some smokers find helpful.

The product is not a true inhaler in that nicotine is not delivered to the bronchi or lungs, but rather deposited and absorbed in the mouth, much like nicotine gum. The majority of nicotine is delivered into the oral cavity (36 %) and the oesophagus and stomach (36 %), with very little nicotine reaching the lung.

The recommended dose is between 6 and 16 cartridges a day, for up to 6 months. Depth of inhalation does not appear to be a major determinant of dosing. The amount of nicotine absorbed from the inhaler is temperature-dependent, with higher ambient air temperatures delivering larger amounts of nicotine.

The most common side effects, especially when first using the inhaler, include:

• Coughing
• Throat irritation
• Upset stomach

At this time, inhalers are the most expensive of the forms of NRT available.

Nicotine lozenges

These are the newest form of NRT on the market. As with nicotine gum, the lozenge is available in different strengths: 1 mg, 2 mg and 4 mg. Smokers determine which dose is appropriate, based on how long after waking up they normally have their first cigarette.

The lozenge manufacturer recommends using it as part of a 12 week program. The recommended dose is one lozenge every 1-2 hours for 6 weeks, then one lozenge every 2-4 hours for weeks 7 to 9, and finally, one lozenge every 4-8 hours for weeks 10 to 12. In addition, the manufacturer recommends the following:

• Stop all tobacco use when beginning therapy with the lozenge.
• Do not eat or drink for 15 minutes before using the lozenge. (Some beverages can reduce the effectiveness of the lozenge).
• Suck on the lozenge until it dissolves. Do not bite or chew it like a hard candy, and do not swallow it.
• Do not use more than 5 lozenges in 6 hours, or more than 20 lozenges total per day.
• Stop using the lozenge after 12 weeks. If you still feel you need to use the lozenge, talk to your doctor.
• Do not use the lozenge if you continue to smoke, chew tobacco, use snuff or any other product containing nicotine (e.g., nicotine patch or gum).

Possible side effects of the nicotine lozenge include:

• Trouble sleeping
• Nausea
• Hiccups
• Coughing
• Heartburn
• Headache
• Flatulence (gas)

NiQuitin, Nicotinell are examples of lozenges and dissolve on the tongue.

Nicotine microtabs

Microtabs are tiny tablets that are placed under the tongue and release nicotine slowly as they dissolve. They are ideal if one gets cravings in response to stress or in certain situations. There is only one strength of microtabs, 2 mg, and one should not use more than two per hour. The aim is to reduce the number you use every day over period of thee months, until you have stopped craving nicotine and do not need to rely on them. Microtabs are only available from behind the pharmacy counter.

Nicotine vaccines

There are at least three companies in early development of an antinicotine vaccine: Xenova (TA-NIC), Nabi (NicVax) and Cytos (Nicotine-Qbeta). Results of Phase I studies on TA-NIC and Nicvax reported as conference abstracts suggest that these vaccines are safe, well tolerated and immunogenic. Preliminary results of the Phase II study indicate the strength of the immunological response to the vaccine varies among individuals. Among individuals with antibody responses in highest tertile, continuous abstinence rates were significantly lower than among subjects who received a placebo vaccine.
A vaccine against nicotine induces antibodies against the nicotine molecule that prevents the drug from reaching neural receptors that produce the effects normally associated with smoking.

NON- NICOTINE AID

Bupropion - ZYBAN

Image 2: Bupropion.

Bupropion hydrochloride (ZYBAN) sustained-release tablets are a non-nicotine aid to smoking cessation. Bupropion is chemically unrelated to nicotine or other agents currently used in the treatment of nicotine addiction. It is a relatively weak inhibitor of the neuronal uptake of norepinephrine and dopamine, and does not inhibit monoamine oxidase or the re-uptake of serotonin. The mechanism by which bupropion enhances the ability of patients to abstain from smoking is unknown. However, it is presumed that this action is mediated by noradrenergic and/or dopaminergic mechanisms. The recommended and maximum dose of bupropion is 300 mg / day, given as 150 mg twice daily. Dry mouth and insomnia are the most common adverse events associated with use.

Varenicline – CHAMPIX, nicotine receptor antagonist

Image 3: Varenicline.

Varenicline (Champix in ROI) is a newer medicine developed specifically to help people stop smoking. It works by interfering with nicotine receptors in the brain, which has two effects. It lessens the pleasurable physical effects a person gets from smoking, as well as reducing the symptoms of nicotine withdrawal.

Several studies have shown varenicline can more than double the chances of quitting smoking. Some studies have also found it may be more effective than bupropion, at least in the short term.

It differs from bupropion, an anti-depressant which had been on the market for many years. The neurochemistry of varenicline is complex. It is a nicotinic acetylcholine receptor partial agonist. That means that it has both a stimulating and a blocking effect on the receptor it is attracted to. It is structurally similar to cytosine, a naturally occurring substance used as a starting point to develop varenicline. Cytosine has been licensed as a stop smoking medication for around 40 years in Central and Eastern Europe.

Agonist means that when varenicline binds to the nicotinic receptor it has an effect similar to that of nicotine in stimulating the release of dopamine, although varenicline produces a slower, longer lasting and smaller increase in dopamine release than nicotine. Thus it partially mimics the effect of nicotine and this is thought to explain why it reduces craving when smokers abstain and are deprived of nicotine. However varenicline also binds to the receptor and partially blocks it (hence “partial agonist”), which reduces the binding site availability for nicotine, and so results in a weaker response if people smoke while using the drug.

“Five day plan”: quitting smoking through acceptance of addiction and realization of smoking’s harmfulness

“Five day plan” is one of the oldest and most effective smoking cessation programs to date. It was first published by J. Wayne McFarland, M.D. and elman J. Folkenberg in 1964.

The program takes participants through a five-day, step-by-step program to change daily habits and achieve their goal to quit smoking. Through psychological motivations, such as affirmation statements, and physical changes, such as dietary modifications, the Five-day Plan works to break the participant’s cigarette cravings and smoking routine.

You can find more information on the web site of University Health Services or by following this link.

OTHER (ALTERNATIVE) METHODS OF QUITTING

Other tools may also help some people, although there is no strong evidence they can improve ones chances of quitting.

Atropine and scopolamine combination therapy: Some smoking cessation clinics offer a program using shots of the anticholinergic drugs atropine and scopolamine to help reduce nicotine withdrawal symptoms. These drugs are more commonly prescribed for other reasons, such as digestive system problems, motion sickness, or Parkinson’s disease.

The treatment usually involves injections given in the clinic on one day, followed by a few weeks of pills and wearing patches behind the ear. It may include other drugs to help with side effects as well.

Possible side effects of this treatment can include dizziness, constipation, dry mouth, an altered sense of taste and smell, problems urinating, and blurry vision. People who are pregnant or have a history of heart problems, glaucoma, or uncontrolled high blood pressure are not allowed to participate in these programs.

Some clinics claim high success rates, but there is no published scientific research to back up these claims. Both atropine and scopolamine are approved for other uses, but they have not been formally studied or approved for help in quitting smoking. Before considering such a program, you may want to ask the clinic about long-term success rates (up to a year). Because these medicines are directed only at the physical aspect of quitting, you may also want to ask if the program includes counselling or other methods aimed at the psychological aspects of quitting.

Hypnosis might be useful for some people.

Acupuncture has been used for quitting smoking, but there is little evidence to support its effectiveness. Acupuncture, when it is done, is typically done on the ears on particular ear sites. Although there is a very weak suggestion that acupuncture might lower the desire for smoking, there still is no solid evidence that it is truly effective as a smoking cessation tool.

Low level laser therapy, also called cold laser therapy, is a related technique. Cold lasers are sometimes used for acupuncture, with laser beams to stimulate the body's acupoints rather than needles. The treatment is supposed to relax the smoker and release endorphins (naturally-occurring pain relief substances) in the body to simulate the effects of nicotine in the brain, or balance the body’s energy to relieve the addiction. Despite claims of success by some cold laser therapy providers, there is no scientific evidence that shows this is an effective method of helping people stop smoking.

Filters that reduce tar and nicotine in cigarettes are generally not effective since studies have show that smokers who use filters actually tend to smoke more.

Smoking deterrents such as over-the-counter products that change the taste of tobacco, "stop smoking diets" that curb nicotine cravings, and combinations of vitamins have little scientific evidence to support their claims.

The same is true of “homeopathic” aids and herbal supplements. Because they are marketed as dietary supplements (as opposed to drugs), they don’t need approval to be sold. The manufacturers don’t have to prove they’re effective, or even safe. Be sure to look closely at the product label of any product claiming it can help you stop smoking. No dietary supplement has been proven effective in helping people quit smoking. Some of these supplements have no nicotine in them, but have multiple combinations of herbal preparations. They too have no proven track record of helping people to stop smoking.

Nicotine water and nicotine wafers: These products have been sold in recent years as ways to get nicotine in places where smoking is not permitted. They are not marketed as aids to quitting smoking, but questions about their safety and legality have been raised.

WHICH TYPE OF NRT TO CHOOSE?

When choosing which type of nicotine replacement to use, think about which method will best fit your lifestyle and pattern of smoking. Do you want/need something to chew or occupy your hands? Or are you looking for once-a-day convenience? There is no evidence that any type of nicotine replacement therapy is significantly better than any other.

Some important points to consider:

• Nicotine gums, lozenges, and inhalers are oral substitutes that allow you to control your dosage to help keep cravings under better control.
• Nicotine nasal spray works very quickly when you need it.
• Nicotine inhalers allow you to mimic the use of cigarettes by puffing and holding the inhaler.
• Nicotine patches are convenient and only have to be applied once a day.
• Nasal sprays require a doctor’s prescription (not available in ROI).
• Some people may not be able to use patches, inhalers, or nasal sprays due to allergies or other conditions.

Combination of the patch and other nicotine replacement products

Using the nicotine patch along with shorter-acting products such as the gum, lozenge, nasal spray, or inhaler is another method of nicotine replacement therapy. The idea is to provide a steady dose of nicotine with the patch and to use one of the shorter-acting products when strong cravings arise.

The few studies that have been done on combination NRT have found that it may be slightly better than a single product, but more research is needed to prove this and to find safe and effective doses. If you are considering using more than one nicotine replacement product, be sure to discuss this with your doctor first.

High-Dose Nicotine Replacement Therapy

One of the newer concepts in nicotine replacement therapy is to give smokers a higher dose specifically titrated to the amount of nicotine that they have been using. Sometimes this method has required larger doses of nicotine than have been used traditionally in the past. High-dose nicotine replacement therapy with patches has been studied with patients receiving from 35 mg to 63 mg of nicotine at a time. The research suggests that patients' withdrawal symptoms disappear with these higher doses and their cravings decrease without any adverse cardiovascular side effects. Patient were carefully monitored in these studies to make sure they were doing well and were not becoming ill or having any problems. This is still a new procedure that should be considered only with a doctor's guidance and supervision.

AFTER GIVING UP SMOKING

Simple lifestyle changes will boost mood and willpower. Once you have quit, the excuses to light up again will come. It is important to come up with different activities that are constructive and help take the mind off cravings.

Healthy food

A healthy diet with plenty of fresh fruit and vegetables provides valuable nutrients that help your body repair faster and rises your immunity. Consider taking a multivitamin and mineral supplement. Some smokers tend to skip meals and the may need to build up certain nutrients. B vitamins may also help maintain energy levels and counteract the stresses and strains of everyday life.

Physical activities

A good way to help lift one’s mood and avoid weight-gain after giving up smoking.

Reward yourself

Give yourself a pat on the back for every day you do not smoke. Treat yourself with the money you save.