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
What is the proposed MOA of Acamprosate (Campral) in alcohol abstinence?
May restore the balance of glutamate and GABA neurotransmitters that is altered d/t chronic alcohol abuse
Acamprosate (Campral) does not cause alcohol _______ .
aversion
also lacks antidepressant, anxiolytic, anticonvulsant activity
What is Dronabinol (Marinol) and who is approved for?
Synthetic THC available for appetite stimulation and antiemetic properties in AIDS and chemo patients
Cocaine’s intense euphoric effects are secondary to blocking reuptake of ______ with lesser effects on ______ and ______ .
Dopamine
NE and 5HT
Which type of drugs have been linked to decrease cocaine cravings?
Antidepressants- desipramine and fluoxetine
MDMA/Ecstasy acts on what neurotransmitter?
5HT, causes release into the synaptic cleft, inhibits synthesis, and inhibits reuptake
(can result 5HT store depletion)
Which benzo is often used in ETOH abuse and withdrawal and why?
Diazepam (Valium) is beneficial due to fast onset and long 1/2 life
(other benzos with long 1/2 life, clonazepam, chlordiazepoxide)
Benzos least likely to cause DI?
Lorazepam
Oxazepam
Temazepam
