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118 Cards in this Set
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- Back
- 3rd side (hint)
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Define Tolerance
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Altered physiological state, where the same dose of a substance has less effects over time. Dose needs to be increase over time to maintain effects.
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Physiological state
Time Dose |
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Behavioral Tolerance
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Behavior to compensate drug effects eg. take another
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Functional Tolerance
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Compensatory changes in receptors, effector enzymes, membrane actions of drugs
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Why is smoking a good way to take some of these drugs
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Rapid effect (onset and elimination)
Can titrate with smoking, take until feel effects and then stop. With smoking, ctrl it so can't OD. With smoking, can breathe out if too much. Don't need clean needles, no complication of skin infections |
Effect (time)
Adv. over other means |
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List 4 biological causes of Tolerance
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Pharmacokinetic
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Main clinical effects of Opioids
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Euphoria
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Drug used for Heroin detox
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Methanol
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Name opioid contained in Tylenol
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Codeine
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Toxidrome for opioid toxicity:
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Depressed mental status
Depressed Resp. Status Mioisis |
3
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Antidote for opioid toxicity
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Naloxene
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True or False
Babies born to opioid addicted mothers may have neurological complications that look like Sz. They can die from this |
True
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How is a pregant heroine addicted mother treated?
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Admit!
Methadone |
Admit for the sake of the baby.
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Symptoms of Heroine withdrawal.
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Look like have flu and don't feel well.
Anxiety, fever, lacrimation, rhinorrhea, sweat, insomnia, weak, chills, myalgia, hypertension, yawn. Rx. Supportive treatment, don't admit. |
Dvp 8 -10 hrs after stop drug
Won't kill them |
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How can treating heroin toxicity lead to withdrawal symptoms?
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If addicted and treat with nalaxone, similar immediate stop of drug.
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List 4 sedative/hypnotic drugs:
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Alcohol
Benzos Barbituates Gamma Hydroxy butyrate |
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What are the symptoms of sedative/ hypnotics toxicity
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Depressed mental statuse
Depressed Resp. rate *** |
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True of False
Withdrawal from sedative/ hypnotics can be life threatening. |
True
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List withdrawal symptoms from benzodiezapines
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Anxiety
Tremors Nausea Vomit SEIZURES |
withdrawal over 8-9 days, may be shorter depending on type of drug or how long it was taken for.
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What is a Rum fit?
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Sz from alchohol withrdawal that occurs in about 1-2hr
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Alchohol withdrawal symptoms:
Mild form (1-2 days) |
Motor agitation
Anxiety Insomnia Sz |
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Alchohol withdrawal symptoms:
Severe form (3-4 days) |
Visual hallucinations
Total disorientation Tachycardia hypertension hyperthermia Sz |
DELIRIUM TREMENS
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Treatment for sedative-hypnotic withdrawal.
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Supportive - prevent Sz
Replace electrolytes Replace thiamine (B1) Admit for severe withdrawal Drug substitution and taper with time |
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What would you give to treat alchohol withdrawal?
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Benzos
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What would you give to treat GBH withdrawal?
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Benzos
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Acute ETOH intoxication may cause death directly from?
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Respiratory Depression
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What system is involved in 90% of metabolism of ETOH to acetaldehyde?
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Alchohol dehydrogenase
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Name the enzyme that breaks down acetaldehyde:
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Aldehyde dehydrogenase
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What serum alchohol is legal limit for driving?
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80mg/dl
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True or False
ETOH is Tissue paralles ETOH in blood |
True
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What system, other than the dehydrogenase system is involved in ETOH metabolism?
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p450 system
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Proof = ? alchohol %
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1/2
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What effect does ETOH have on:
GABA activity Glutamate activity |
Binds GABA receptors and augments GABA activity.
Decreases glutamate activity on its receptors. |
CNS depressant
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Which of these is a chronic effect of alchohol that is reversible?
Wernicke encephalopathy Korsakoff pyschosis/syndrome |
Wernicke Encephalopathy
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As a result of thiamine deficinency
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3 main clinical features Wernicke encephalopathy:
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Depressed mental status
Wide based gait Eye findings: Nystagmus & or intranuclear opthalmoplegia - can't track past midline. |
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clinical features of Korsakoff pyschosis/syndrome
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Short-term memory loss
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Alchoholics are likely to have Cerebral atrophy. Why is this a concern?
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If have head injury, have high risk for subdural hematoma due to stretch of bridging veins.
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Also a concern in elderly patients if see change in mental status that can't explain.
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Major effects of ETOH on Liver:
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Chronic - cirrhosis
Acute: CYP450 induced Chroni: Liver damage reduces drug metabolizing capacity. |
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Major effects of ETOH on stomach:
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Low ETOH: stimulate acid secretion
Chronic ETOH: Mucosal damage and bleeding |
Dose dependent
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Major effects of ETOH on cardiovascular system:
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Dilates blood vessels by depressing vasomotor center
Lead to heat loss - hypothermia Chronic use-myocardial damage |
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Major effects of ETOH on Kidney:
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Diuresis - ETOH reduces ADH secretion.
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Teratogenic effects due to ETOH:
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Fetal alchohol syndrome
CNS impairment Facial abnormalities |
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Major effects of ETOH on pancrease:
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Pancreatitis
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Major effects of ETOH on sexual perfomance:
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Low dose - remove inhibitions
High dose - less performance |
Dose dependent; for both sexes
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List drugs that interact with alchohol:
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Drugs that can irritate stomach not used with ETOH - eg. NSAIDS.
ETOH & Acetaminophen - liver damage at high doses |
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Therapeutic use of ETOH:
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Skin anti-infective
Treat Trigeminal neuralgia Ethylene glycol and ethanol |
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Treatment of alchoholism
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Supportive
Are they breathing? Chance of respiratory depress. Correct hypoglycemia - usually in pediatrics Give thiamine Rule out trauma Drug substitution & taper |
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Which of these patients say take less than they do?
Methadone Alcholic |
Alcoholics - in denial
Methadone patients - say they take more, because they want more while in hospital. |
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What is the MOA of disulfiram?
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Blocks aldehyde dehydrogenase. If drink, have build of of acetaldehyde, responsible for miserable side effects.
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Antabuse
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Name two other susbtances that have disulfiram like activity and should not be used with ETOH
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Cochrine muschrooms
Flagil - metronidazole |
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What are clinical characteristics of methanol toxicity?
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Intoxication
Severe acidosis Blindness Coma Death |
Windshield washer fluid.
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What are clinical characteristics of Ethylene glycol toxicity?
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Intoxication
Severe acidosis Renal failure Coma Death |
Anti-freeze
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Define Sedatives-hypnotics
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General depressants of the CNS
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Joint definition
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Define Sedatives
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Reduce daytime anxiety
Decr. excessive excitement Promote calm state |
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Define Hypnotics
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Produce drowsiness
Promote onset of sleep Promote maintenance of sleep |
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What effects do alpha-1 subunits of GABA receptors have?
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Sedative and
MEMORY effects ... be mindful of this |
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What is the difference between Benzos and Barbs?
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Benzos a lot safer than Barbs
Benzos level off with increased dose At high conc, barbs may direcly activate channel, may cause death. |
Sedation -- Hypnosis -- Anethesia -- Coma
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Name 4 Short acting Benzos
(Safer - not likely to sleep on road in the morning) |
Lorazepam 0 - 20hr
Oxazepam 0 - 20hr Triazolam 2 - 3hr Alprazolam 12- 15hr |
LOT - these are drugs you want to remember, have no active metabolites!!!
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Name 3 Long acting acting Benzos
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Flurazepam 100hr
Prazepam 100hr Clorazepate 100hr |
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BZD side effects
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Intoxication
Disinhibition Impaired judgement, aggressive Withdrawal - life threatening |
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How are patients who have been on long-half life BZD for more than a year taken off of BZD?
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First 50% withdrawal
Then taper drug by 10% or less per week. |
Long half-life up to 6wks, unlikely for withdrawal
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List side effects of BZD
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Daytime drowsiness
Dizziness Ataxia Resp. impairement in patients with COPD Amnesia, memory impairement |
Patients with COPD
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Effect of BZD with other sedatives
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Coma, increased CNS depression
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Interaction btw. antacids and BZD
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Decreased absorbption of BZD
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List three BZD that are safe to use with Liver problems.
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Lorazepam
Oxazepam Temazepam |
Drugs are conjugated and secreted in the urine
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What effect does Grape juice, estrogens, Isoniazie, Fluoxetine have on BZD levels?
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Also metabolized by the CYP450, therefore Increase BZD levels in blood.
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Metabolism
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Symptoms of insomnia
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Difficulty falling asleep
Difficulty maintaining sleep Frequent awakenings Poor quality sleep Have adequate time to sleep |
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Characteristics of sleep disorder:
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Insomnia and
Distress - daytime sleepiness, mood disturbance, impaired cognition, daytime sleepiness |
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Epidemeology of insomnia:
What % have chronic or occasional insomnia |
30% occasional
10% chronic |
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Define primary insomnia (15%)
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Main problem is insomnia
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Define secondary insomnia (85%)
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Secondary to medical disorder, pyschiatric and other substance abuse, other sleep disorder eg. restless leg syndrome.
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Name 3 behavioral treatments of insomnia
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Relaxation training
Sleep restriction therapy (increase sleep efficiency) Stimulus control therapy |
Good sleep hygiene - caffeine has long half life, none after 12pm
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Effects of behavioral treatments:
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Reduce sleep latency
Reduce wake time after sleep onset Increase total sleep time |
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What is the most frequent antihistamine used to treat insomnia?
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Benadryl: Diphenhydramine
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H1 receptors
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Side effects of Benadryl as hypnotic?
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Cognitive impairement
Confusion Sedation Delirium Urinary retention in elderly |
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What are the drugs of choice for insomnia?
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Benzodiezapine receptor agonists
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List Benzodiezapines that have been approved for the treatment of insomnia:
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Estazolam
Quezapam Temezapam Triazolam Flurazepam |
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List three nonBZD hypnotics that act via alpha subunit of GABA receptor:
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Zolpidem - Ambien 2.5hr
Zaleplon - Sonata 1hr Eszopiclone - Lunesta 6hr |
LESS ABUSE POTENTIAL
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Which drug would you give to a patient with middle of the night insomnia?
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Zaleplon (Sonata)
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How is Ambien metabolized?
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Liver metabolism
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What are the preferred hypnotics?
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BZD, Ambien, Sonata
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Less risk of fatal OD with threse drugs
Barbs not a drug of choice due to use in suicide attempts. |
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What's the difference btwn BZD and non-BZD hypnotics?
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non-BZD are more selective, bind to omega-1 subtype of GABA receptors whereas BZD bind to all three nonselectively.
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Describe the amine hypothesis of depression
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Deficiency of amines (NE and Serotonin) in certain parts of the brain leads to depression.
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Where in the brain are the cell bodies of Noradrenergic tracts?
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Locus Coerulues
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Project to:
Caudate Amygdaloid nucleus Thalamus Hypothalamus Cortex |
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Where in the brain are the cell bodies of Serotonergic tracts?
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Raphe nuclei
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Project to limbic system and cortex
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List 5 SSRI's
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Fluoxetine - prozac
Sertraline - Zoloft Paroxetine - Paxil Citalopram - Celexa/ Escitalopram(Lexapro) Fluvoxamine |
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Describe the char. of serotonin syndrome seen with SSRI's
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Confusion
Fever Altered consciousness Myoclonus |
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MOA of Fluoxetine
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Selective inhibition of serotonin reuptake on presynaptic membrane, allowing longer interaction of serotonin with postsynaptic membrane.
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Advantage of Sertraline over Fluoxetine
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Sertraline has a shorter half life and therefore takes a shorter time to reach steady state. Therefore, it is easier to change patient from sertraline to another drug due to the fact that it gets out of the system faster.
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What are the unique char. of paroxetine?
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Has anticholnergic effects in addition to SSRI, therefore can relieve anxiety.
Side effects: constipation. |
Severe discontinuation syndrome if stopped abruptly
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List the therapeutic use of SSRI's
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Depression
OCD Panic disorders Post traumatic stress disorder Eating disorder Generalized anxiety disorder Premenstrual syndrome |
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MOA of Tricyclic antidepressants.
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They block the active reuptake of NE and serotonin at the presynaptic membrane of NE and serotonin tracts.
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What is the current therapeutic use of Tricyclic antidepressants.
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Treatment of resistant depression.
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Not first line because of high treatment dropout rate due to adverse effects.
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List some adverse effects of Tricyclic antidepressants.
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Sedation
Anticholinergic (urinary hesitancy)**** Orthostatic hypotension ECG changes Weight gain Headache, tremor, Sz Obstructive jaundice Sexual side effects Class1a anti-arrythmic Likely to ppt mania |
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Treatment of poisoning of Tricyclic antidepressants.
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Cardiac monitoring
Gastric lavage Sodium bicarbonate and KCl Lidocaine or Phenytoin I.V. |
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Name the only TCA with clinically proven therapeutic drug level.
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Noretriptyline
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Which TCA interacts with morphine to potentiate morphine analgesic effects.
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Amitryptyline
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What are the therapeutic of TCA
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Depression
Enuresis in childhood Chronic pain, neuralgias, migraine neuropathy |
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What effects of TCA's with anti-htn
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Reverse of anti-htn action
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Which are the original Gold standard drugs that are used to treat depression.
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TCA
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List two noepinephrine and serotonin reuptake inhibitor (SNRI):
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Venlafaxine
Duloxetine |
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Therapeutic use of venlaxafine
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Depression
Generalized anxiety disorder Social Anxiety Disorder Panic disorders PSTD Premenstrual syndrome |
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Duloxetine - How is this different between this and venlaxafine.
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Diabetic peripheral neuropathy
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What is the MOA or Monoamine Oxidase:
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Inhibition of intraneuronal monoamine oxidase type A isoenzyme in noradrenergic and serotonergic fiber tracts.
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List MAO inhibitors:
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Phenelzine - more side effects
Tranylcypromine |
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Side effects of phenelzine:
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*weight gain
*orthostatic hypotension *hepatotoxicity potential *anxielytic Slower onset of action Sexual dysfunction |
Hydrazine derivative
* more than tranlycypromine |
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Side effects of Tranylcypromine:
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sexual dysfunction
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Which MAO inhibitors has faster onset of action and some abuse potential
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Tranylcypromine - a non-hydrazine
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What are the clinical char of an MAOI crisis?
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Hypertensive crisis
headache palpitations sweating Chestpain hemorrhagic stroke |
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What is the outcome of interaction btw. MAOI and Tyramine foods?
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Hypertensive crisis
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What is the outcome of interaction btw. MAOI and meperidine?
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Convulsions, cardiovascular failure and death
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What is the therapuetic use of MAOI's?
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Superior for bipolar disorder than TCA
Phobic anxiety states Migraines Neurodermatitis |
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What class of drugs does Buproprion fall under?
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Noepinephrine and Dopamin reuptake inhibitor (NDRI)
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What is the therapuetic use of Buproprion?
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Depression, fewer sexual side effects than SSRI
Smoking cessation ADHD |
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Name an antidepressant that is used in smoking cessation
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Buproprion
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Drug used to treat ADHD
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Buproprion
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Adverse rxns of Buproprion
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Agitation
Dose dependent risk of Sz headache nause Sz Blurred vission |
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Advantages of SSRI's over TCA
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Do not have quinidine action on heart
Safety margins are higher in OD No need to measure/follow blood levels LAck anticholinergic, antihistamine effects No weight gain |
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Important dietary restriction for patients on MAOI's
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Avoid foods that contain tyramine
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