Tobacco, Alcohol, Benzos Flashcards
Nicotine directly activates _____ _____ receptors. Where:
nicotinic ACh receptors
centrally, peripherally, and at the Nm junction
How much less nicotine do nicotine replacements contain vs. cigarettes?
1/3 to 1/2 less nicotine
Why is nicotine replacement less likely to cause addiction?
It takes a longer type for systemic absorption. Inhaling nicotine allows for very fast entrance to circulation.
OTC Nicotine replacement products include:
Gum (Nicorette)
Lozenges (Commit)
Patch (Nicoderm CQ)
Rx Nicotine replacement products include:
Oral inhaler (Nicotrol inhaler) Nicotine nasal inhaler (Nicotrol NS)
Instructions and SE for nicotine gum:
Keep between cheek and gums, do not chew
SE: tingling on tongue, hiccups, jaw pain, nausea/heartburn if chewed
Instructions and SE for nicotine lozenge:
Do not swallow
SE: HA, flatulence, hiccups, nausea/heartburn if swallowed
Instructions and SE for nicotine patch:
Dose: Stepwise based on number of cigarettes/day
SE: Skin rash, use topical antihistamine
Sleep disturbance, take patch off at night
Instructions and SE for nicotine inhaler:
Avoid in patents with resp. disease, like asthma
SE:cough, scratchy throat, GI upset
Which antidepressant is used for smoking cessation and its presumed MOA?
Bupropion (Zyban)-usually added with nicotine replacement product
Noradrenergic and dopaminergic effects play a role
AE of using Buproprion for smoking cessation:
Difficulty sleeping, issues concentrating, tremors, GI upset
What is Varenicline (Chantix) MOA and AE:
Agonist at a sub-type of the nicotinic ACh receptor
This blocks nicotines activity of the receptor eliminating the reward experience caused by smoking
AE: nausea, HA, insomnia, abnormal dreams
(usually start prior to patient quitting)
What black box warning do Bupropion and Varenicline have?
Serious neuropsychiatric events
Depression- suicidal ideation. Changes in behavior- aggression, hostility, agitation
What receptors does alcohol act on?
GABA (inhibitory)
NMDA glutamate (excitatory)
Cannabinoid
What does GABA mediate?
Anxiolytic and sedative effects as well as muscle coordination, tolerance, and dependence
What is used in the treatment of acute alcohol withdrawal?
Benzodiazepines
What drugs are used in maintenance of alcohol cessation?
Disulfiram (Antabuse)
Acamprosate (Campral)
Naltrexone
Benzos can be used for?
Sleep Anxiety Alcohol withdrawal Seizures Anesthesia
Withdrawal s/s of benzos include:
Anxiety, insomnia, irritability, nausea, blurred vision, confusion, delirium, seizures
What is the advantage of benzos with a longer half-life?
Self-tapering effect= less s/s of withdrawal
The benzos with the least drug interactions include:
Lorazepam
Oxazepam
Temazepam
(not metabolized by the CYP3A4 pathway)
Diazepam (Valium), Alprazolam (Xanax), and Clonazepam (Klonopin) are all metabolized by:
CYP3A4
MOA of Disulfiram (antabuse):
Inhibits aldehyde dehydrogenase, a critical enzyme in the alcohol metabolism pathway. Aldehyde is unable to be broken down to acetic acid and begin to accumulate
S/S of aldehyde accumulation:
Facial flushing, HA, N/V, weakness, orthostatic hypotension