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82 Cards in this Set

  • Front
  • Back

Butalbital

•Barbituate

Thiopental

•Barbituate

Barbituates in general

•Too dangerous due to low therapeutic index •Narrow therapeutic window •Increase open time of the Cl- channel •Tolerance develops to sleep induction, but not to respiratory depression

Benzodiazepines in general

•Non lethal in overdose but cause serious dependence and withdrawal syndromes •Increase open frequency of GABA Cl- channel •Some benzos are metabolized by CYPs, but benzodiazepines do not induce CYPs like Barbituates do

Diazepam

•Benzodiazepine •Treatment for chronic alcohol withdrawal •Used as a muscle relaxant

Alprazolam

•Benzodiazepine

Flurazepam

•Benzodiazepine

Lorazepam

•Benzodiazepine

Midazolam

•Benzodiazepine •Used in pre-op with combination opioid for conscious sedation

Triazolam

•Benzodiazepine •Short T1/2 and forms no intermediates •Contraindicated in pregnancy •Patients taking Triazolam prior to bed may awake w/ rebound insomnia by early AM

Z drugs in general

•Pharmacodynamics very similar to benzos, but adverse effects are less serious •Z drugs are ineffective as anticonvulsants and muscle relaxants •Bind to more restrictive type of GABA-A receptor, those with Alpha1 subunit •All three are schedule IV substances

Eszoplicone

•Z drug •Longest acting, T1/2 = 6 hours •Approved for long term use, effective for latency and maintenance •Dysguesia (altered taste) common with Eszopiclone

Zaleplon

•Z drug •Shortest acting Z drug (1 hr) - dosed right at bedtime or in middle of night if patient wakes up

Zolpidem

•Z drug •Not approved for long term use but is most common Z drug •Hepatic insufficiency doubles half life (2->4 hours)

Ramelteon

•Melatonin receptor agonist •Little potential for dependence of abuse, not a schedule substance •Only small benefits: reduce sleep latency by 5 minutes, increase total sleep by 10 minutes

Suvorexant

•Orexin receptor antagonist •Super shitty patient rating for this drug •Contraindicated in narcoleptics

Cyclobenzaprine

•Muscle relaxant •Not effective for cerebral palsy or spinal cord injury •Should be limited to short term •Not recommended in mild to severe hepatic impairment

Baclofen

•Muscle relaxant •Considered superior to diazepam for spasticity due to similar efficacy, less sedation •Can be used for severe spasticity •Black box warning for abrupt withdrawal •SPASTICITY SPASTICITY SPASTICITY

Tizanidine

•Muscle relaxant •Central Alpha2 agonist •Like Clonidine but much less hypotensive •Side effects = hypotension, drowsiness, xerostomia, hepatotoxicity

Botulinum Toxin

Muscle relaxant Botox penetrates neuron membranes to enzymatically cleave a neuronal protein that is necessary for ACh release, called Synaptobrevin Clinical use of botox in blepharospasm (eyelid spasm) = marked by involuntary, sustained contractions of orbital muscle and photosensitivity Black box warning due to spreading effects that causes weakness in swallowing and breathing muscles, leading to death

Succinylcholine and Vecuronium

Muscle relaxants that work by being antagonists of nicotinic cholinergic receptors in skeletal muscle

Diazepam

•Alcohol drug •Preferred drug for treating serious alcohol withdrawal

Naltrexone

•Alcohol drug


•First line therapy for treating alcohol addiction •Long acting antagonist of mu-type opioid receptor •Do not combine with Disulfiram (causes hepatotoxicity)

Acamprosate

•Alcohol drug •Probably more efficacious in maintaining alcohol abstinence rather than starting it •Can be used safely in individuals with liver impairment, and in those receiving opioids, but avoid in severe renal deficiency

Disulfiram

•Alcohol drug •Inhibits ALDH enzyme •Aversive (meaning alcohol use perpetuates negative feeling which is buildup of acetaldehyde) •Avoided in pregnancy and nursing

Ethyl Alcohol

•Booze is sick •Eliminated by zero order kinetics •East Asiants are more likely to have deficient ALDH2, or unusually rapid alcohol dehydrogenase •Mellanby effect: impairment at a given BAC is greater when BAC is rising than when BAC is falling •All patients presenting to ER with altered consciousness receive thiamine to prevent Wernicke-Korsakoff syndrome (thiamine def seen frequently in alcoholics) •Distribution of alcohol in the body tends to follow that of body water

D-amphetamine

•Psychomotor stimulant •The D isomer of amphetamine exerts a greater effect in the CNS

Lisdexamfetamine

•Psychomotor stimulant •Prodrug in which amphetamine is linked to Lys •Moderate rate of conversion to amphetamine supposedly limits abuse potential

Methamphetamine

•Psychomotor stimulant •Speed-crank-ice (Ice is the crystalline smokeable form •The presence of the methyl groups makes the drug resistant to metabolism by MAO and increases its lipid solubility •Produces very intense effects in the CNS and is widely abused

Methylphenidate

•Used for treatment of ADD in children •The primary site of action is the locus ceruleus which contains most of the NE producing neurons of the brain

Cathinone

•Psychomotor stimulant •Found in leaves of the khat plant, a shrub indigenous to Eastern Africa and parts of the middle east •Cathinone analogs such as methylenedioxoprovalerone are easy to synthesize and have been used in products labeled as bath salts

Ephedrine

•Psychomotor stimulant •Natural product found in herbal preparations •Used medically as a sympathomimetic agents •Can be used as an ingredient to make amphetamine

Modafanil and Armodafanil

•Psychomotor stimulant •Newer non-amphetamine stimulants approved for the treatment of narcolepsy and shift work disorder •They do have many amphetamine like effects

Cocaine

•Psychomotor stimulant •CNS stimulation, euphoria and a sense of well being, reinforcing effects on reward centers, suppression of appetite, paranoia, hallucinations •MOA = inhibition of synaptic reuptake of NE and DA results in stimulant and reinforcing effects respectively •Symptoms of withdrawal commonly include depression

Caffeine and related methylxanthines in general

•Psychomotor stimulant •Naturally occurring compounds •Stimulation of gastric secretion = avoid use in patients with peptic ulcer disease Methylxanthine overdose is characterized by excessive CNS stimulation which can result in life threatening seizures •MOA = 3 biochemical effects: inhibition of phosphodiesterase, blockade of adenosine receptors, release of Ca2+

Theophylline

Methylxanthine used in treatment of asthma

Aminophylline

Methylxanthine used in treatment of Severe asthma

Strychnine

•Methylxanthine •Potent convulsant used as a rat poison (acts as antagonist at glycine receptors in the spinal cord and other areas of the CNS •Treatment consists of symptomatic support plus the use of Diazepam to control seizures •Thought to cause seizures by antagonizing the synaptic actions of glycine

Tetanus toxin

•Methylxanthine •Released by Clostridium tetani during infection •Acts by inhibiting the release of glycine from Renshaw cells in the spinal cord and other areas •Treatment consists of symptomatic support, Diazepam for the control of seizures, and appropriate antimicrobial therapy

What do Theophylline and Caffeine sometimes treat in preterm infants?

Apnea

Adderall is a Methamphetamine drug that is an ________ ___________.

Extended release

Amphetamine

•Psychomotor stimulant •Increases level of arousal and wakefulness via stimulation of reticular activating system; enhanced sense of confidence and well being, delay of fatigue induced decline in performance •Toxicity = Sympathomimetic effects: CNS, cardiovascular, and potential for irreversible degeneration of dopaminergic and serotonergic pathways in the brain •MOA = Enhanced release and inhibition of the uptake of NE and DA; possible direct stimulation of alpha receptors in reward center of brain •Used for narcolepsy, ADD, Obesity and weight reduction

Haloperidol

•Hi potency first generation antipsychotic •Black box warning for QT prolongation, TdP and ventricular arrhythmias •Strong D2 affinity, low cholinergic and adrenergic affinity •High risk of EPS, Some H1 antagonism = some sedation and weight gain •Symptoms of Tardive dyskinesia can be suppressed by high doses of Haloperidol

Perphenazine

•High potency first generation antipsychotic •Slightly less EPS and hyperprolactinemia than haloperidol •Strong H1 antagonism yields high weight gain

Chlorpromazine

•Low potency first generation antipsychotic •Most commonly used low potency FGA •Strong Anti ACh block/alpha1 block •High tendency to cause nausea as a side effect

Thioridazine

•Low potency first generation antipsychotic •FDA blackbox for Thioridazine: of all antipsychotics, most commonly associated with long QT and TdP

Aripiprazole

•Second generation antipsychotic •Exceptionally high affinity for D2 (even higher than Haloperidol and other hi potency FGAs) •Gentle toxicity profile despite high D2 affinity •$$$$$$$$$

Clozapine

•Second generation antipsychotic •Recognized for a very low rate of TD •Stands apart from all other antipsychotics •Effective in schizophrenia accompanied by persistent suicidal or self injurious behavior •Tobacco smoke induces CYP1A2 = smokers may require 2x dose Causes excessive drooling •Also causes Urinary incontinence •Black box warning for 5 toxicities: 1. Agranulocytosis (WBC monitoring), 2. Orthostatic hypotension, bradycardia, syncope, 3. Seizures, 4. Myocarditis and cardiomyopathy, 5. Increased mortality in elderly patients with dementia-related psychosis •Effective in treatment of schizophrenia secondary to parkinson's treatment

Olanzapine

•SGA with strong/highest weight gain and metabolic effects •Possible efficacy against some of the negative symptoms of schizophrenia

Risperidone

•SGA that is commonly used •Carries highest risk of EPS and hyperprolactinemia of all SGAs

Ziprasidone

•SGA •Low risk of weight gain and metabolic disorder

Citalopram

•SSRI

Fluoxetine

•SSRI •Withdrawal symptoms rarely occur with Fluoxetine because of its long duration of action •Treatment of depression, bulimia nervosa, OCD, premenstural dysphoric dysorder

Sertraline

•SSRI

Venlafaxine

•SNRI •Prominent withdrawal symptoms after suddent cessation due to short half life of drug

Duloxetine

•SNRI •Moderate inhibitor of CYP2D6

Imipramine (Im in the Teen Choice Awards)

•TCA •Enuresis in children, pain associated with peripheral neuropathy, migraine, depression

Amitriptyline (taking a -trip- to the Teen's Choice awards)

•TCA

Trazodone

•5-HT antagonist •Blocks serotonin receptor subtypes •Declining use due to rare hepatic toxicity •Non selectivity results in blockage at alpha1 = orthostatic hypertension

Mirtazapine

•Misc. affective disorder drug •Enhances release of 5-HT and NE, also antagonist at some 5-HT and alpha receptors

Buproprion

•Misc. affective disorder drug •Blocks NET and DAT and may cause release of NT's from presynaptic vesicles •Low incidence of sexual side effects •CONTRAINDICATED IN SEIZURE DISORDER, ANOREXIA AND BULIMIA



Tranylcypromine (PROMI(S)E ME MAO)

•MAOI •Has antidepressant properties •Can produce orthostatic hypertension •Nonselectively inhibits monoamine oxidase A and B •induce hypertensive crises when aged cheese, beer or pickled herring is ingested

Selegiline

•MAOI available in skin patch form which spares GI MAO activity

Lithium

•Mood stabilizer •Drugs that alter kidney function can importantly alter Li+ levels (thiazides, NSAIDS (aspirin safe), ACE inhibitors/ARBs) •In severe cases of toxicity, dialysis is the most effective means of removing Li+ •Li+ decreases ADH effect on kidney and reduces ability to excrete urine •Severe Li+ poisoning can be irreversible and SILENT = Syndrome of Irreversible Lithium Effectuated Neurotoxicity •In treatment of bipolar disorder, more effective against the manic phase than against the depressed phase •Retention of lithium is enhanced by a low sodium diet •Early signs of lithium toxicity include nausea, vomiting, slurred speech

All antidepressants carry a blackbox warning for increased chance of suicide in use of those under the age of _ _.

24

MAOIs in general

•Agents of last resort •Inhibit degradation of NT •Inhibition is usually irreversible Most serotonergic antidepressants should be discontinued at least 2 weeks before MAO therapy and vice versa (except Fluoxetine [because of longer t1/2] should be stopped 5 weeks before MAOI) •Has antidepressant properties •Has antidepressant properties •Can produce orthostatic hypertension •Nonselectively inhibits monoamine oxidase A and B •induce hypertensive crises when aged cheese, beer or pickled herring is ingested

TCAs in general

•Inhibit both SERT and NET •Antagonize multiple targets: H1, ACh, Alpha1, lower seizure threshold •Dangerous: weekly supply is sufficient for suicide; OD = dilated pupils and cardiac arrhythmias

SNRIs in general

•Inhibit both SERT and NET •Used when SSRIs have failed

SSRI in general

•Selective serotonin reuptake inhibitors •Relative lack of affinity for H, ACh and alpha adrenergic receptors •Little abuse potential, but sudden withdrawal symptoms •MOA = downregulation and desensitization of various 5-HT receptor subtypes in presynaptic and postsynaptic locations •signaling in lower spinal cord decreases libido and function

Lysergic and Delthylamine (LSD)

•Hallucinogen (indole) •Heavy LSD usage has been shown to be associated with long term changes in the processing of visual information --> called Hallucinogen persisting perception disorder

Psyilocybin and psilocin

•Hallucinogen (indole) •Found in hallucinogenic mushrooms

Bufotenin

•Hallucinogen (indole) •Found in some mushrooms and in the skin of some amphibians

Ibogaine

•Hallucinogen (Indole) •Alkaloid found in the roots of an African shrub •Powerful hallucinogen that has recently been reported to suppress the craving for heroin, cocaine and other drugs in addicted individuals

Dimethyltryptamine (DMT)

Hallucinogen (Indole)


Phenylethylamines - Hallucinogens in general

Have hallucinogenic actions but also produce amphetamine like stimulant effects

Mescaline (The Mesca desert out in Arizona, I found a hallucinating cactus)

•Hallucinogen (Phenylethylamine) •Found in buttons of peyote cactus, effects are similar to those of LSD but the somatic and autonomic changes are more pronounced

Methylenedioxymethamphetamine (MDMA)/MOLLY/ECSTASY

Hallucinogen (phenylethylamine) •Now one of the more common hallucinogens

Phencyclidine (PCP)

•Hallucinogen (phenylethylamine) •Low doses produce effects similar to those of marijuana •At higher doses, hallucination, psychotic reaction and rage reactions occur •Psychotic reactions more common than with other drugs •Enhanced feeling of strength with inability to feel pain •Symptom of acute poisoning: Vertical Nystagmus = looking upThought to produce major CNS effects by acting at NMDA receptors

Ketamine

•Hallucinogenic (phenylethylamine) •Dissociative anesthetic that is used in humans and animals •It resembles phencyclidine in many respects and is not being diverted for abused purposes and is a popular club drug

Marijuana

...... Know it you idiot

Flumazenil

•Benzodiazepine receptor Antagonist •Can reverse the sedating effects of benzodiazepines and Z drugs •IV only •Most useful in reversign Midazolam effects (preop) •Avoid in patient with underlying seizure disorder, or taking other drugs that lower the seizure threshold

Caffeine

•Constriction of cerebral blood vessels •Diuretic effect •Increased level of mental arousal •Stimulation of gastric acid secretion •dilation of bronchial smooth muscle