Drug
Benzodiazepines |(sedatives & hypnotics) | |
|Diazepam (Valium) |Long-acting |Muscle injuries, MS & CP |CI—pregnancy & nursing (cleft |10X less potent than Xanax |
| |(IV or IM dose) |Status epilepticus |palates) |1st prescription until 1992 |
| | |EtOH withdrawal | |10s onset (MOST lipophilic) |
|Clorazepate |Long-acting |Partial seizures | |Combo w/ anti-convulsants |
| | |EtOH withdrawal | |Decarboxylated in stomach |
|Clonazepam (Klonopin) |Long-acting |Panic disorder |Tolerance w/in 1-6m | |
| | |Phobic disorders (2nd-line) | | |
| | |Spasticity (w/o sedation) | | |
| | |Absence seizures | | |
|Flurazepam |Long-acting |Insomnia (inpatients, up to 4w) |Daytime sedation |t1/2 > 100h |
| | | |CI—sleep apnea, snorers | |
|Lorazepam (Ativan) |Intermediate-acting |GAD (2nd) |Safe for elderly & liver dz |2-3min onset |
| |(IV or IM dose) |Status epilepticus |(NO active metabolite) | |
|Alprazolam (Xanax) |Intermediate-acting |DOC for GAD | |10th prescription in US |
| | |Panic disorder (higher doses) | | |
| | |Phobic disorder (2nd-line) | | |
|Temazepam |Intermediate-acting |Insomnia (w/ frequent waking) |Safe for elderly & liver dz |Peaks 2-3h after oral dose |
| | | |(NO active metabolite) | |
| | | |CI—sleep apnea, snorers | |
|Oxazepam |Short-acting |Anxiety, EtOH withdrawal |Safe for elderly & liver dz | |
| | | |(NO active metabolite) | |
|Triazolam |Short-acting |Insomnia (falling asleep) |Tolerance (ONLY 7-10d), rebound |MOST potent (4X Xanax) |
| | | |insomnia, REM rebound, amnesia, | |
| | | |disinhibition | |
|Midazolam |Ultra-short-acting |Pre-op anesthesia, |CI—narcotics & COPD |NOT general anesthesia |
| | |oral surgery | | |
|Flumazenil |Benzo antagonist |Benzo overdose | | |
| |(IV dose ONLY) |Rx for sedation | | |
|Buspirone |5-HT1A agonist |Selective anxiolytic |NO dependence or WD |NOT muscle relaxant OR |
| | |(elderly & alcoholics) |NO interaction w/ EtOH |anti-convulsant |
| | | | |Slow 2-4w onset |
|Zolpidem (Ambien) |Benzo receptor agonists |Selective hypnotic |Minimal rebound insomnia | |
|Zaleplon (Sonata) | | |Interacts w/ EtOH | |
| | | |NO WD or REM effects | |
| | | | | |
|Anti-depressants | | | | |
|Nortryptaline |TCAs |Refractory depression (1st-line) |Anti-cholinergic (esp. elderly), | |
| |(block reuptake of 5-HT & NE) | |sedation (anti-histamine), | |
| | | |seizures, hypotension, | |
| | | |arrhythmias, falls | |
|Sertraline (Zoloft) |SSRIs |MDD |N/D, activating, weight gain, |t1/2 = 26h |
| |(block reuptake of 5-HT) | |sexual dysfxn (30-50%), | |
| | | |5-HT syndrome (combo w/ MAOIs) | |
| | | |LEAST inhibits P450 | |
|Paroxitine (Paxil) |SSRIs |MDD |LESS GI upset, anti-cholinergic, | |
| | | |extra-pyramidal effects, | |
| | | |MOST sexual dysfxn | |
|Fluoxetine (Prozac) |SSRIs |MDD |MOST activating |t1/2 = 192h |
| | | |MOST inhibits P450 | |
|Phenelzine |MAOIs |Reserved for atypical depression |Food (tyramine) OR Pseudoephedrine| |
| |(block degradation of 5-HT & NE) | |( HTN crisis, headaches, | |
| | | |arrhythmias | |
|Bupropion (Wellbutrin) |Blocks reuptake of 5-HT, NE, & DA| | | |
|Hypericum |Inhibits MAO & reuptake of 5-HT &|1st-line MDD in Germany | | |
|(St. John’s Wort) |NE | | | |
|Nefazadone |Blocks reuptake of 5-HT | |Liver toxicity | |
|Trazadone |Strongly blocks reuptake of 5-HT | |Sedative in elderly |Short t1/2 |
|Venlafaxine |Strongly blocks reuptake of 5-HT | |LESS SE than TCAs | |
| |& NE (like TCA) | | | |
| | | | | |
|Anti-psychotics | | | | |
|Chlorpromazine |Phenothiazines | |Anti-cholinergic, anti-NE, | |
| |(DAR antagonist & | |anti-histamine, PD-like effects | |
| |(-blocker) | |sedative | |
|Thioridazine |Phenothiazines | |MORE anti-cholinergic | |
| |(anti-cholinergic) | |LESS sedative & PD-like effects | |
|Fluphenazine |Phenothiazines |MOST potent |LESS sedative | |
| |(w/ 3 halogen substituents) | |MORE PD-like effects | |
|Haloperidol |Typical anti-psychotic | |LESS sedative, LESS cholinergic |Eliminated in bile |
| |(NOT phenothiazine) | |MORE PD-like effects | |
|Clozapine |Atypical anti-psychotics |Low potency |Anti-cholinergic, LESS PD-like | |
| |(blocks 5-HT, NOT D2R) | |effects, agranulocytosis (rare) | |
|Risperidone |Atypical anti-psychotics | |LESS PD-like effects, | |
| |(blocks 5-HT & DAR) | |minimal sedation | |
| | | | | |
| | | | | |
| | | | | |
|Parkinson’s Disease | | | | |
|Benztropine |Anti-cholinergics |Moderate PD (esp. in young) |Dry mouth, blurred vision, |Synthetic derivative similar to|
|Trihexyphenidyl |(1st drugs for PD) |NOT for bradykinesia |cognitive impairment, |Atropine |
| | | |hallucinations | |
| | | |CI—glaucoma, heart dz, GI | |
| | | |obstruction | |
|L-DOPA |(bypasses rate-limiting step of |Best in first 2-5y |Orthostatic hypotension, |95% metabolized by COMT or |
| |DA synthesis) |NOT for cognitive decline |arrhythmias, GI upset, accelerated|L-AAD in periphery |
| | | |cell loss?, | |
| | | |abnormal movements & behavior | |
|Carbidopa (Lodosyn) |Inhibits L-AAD in periphery |(L-DOPA dose by 75% |LESS SEs |Combo w/ L-DOPA (Sinemet) |
| |(prevents L-DOPA metabolism) | | |NOT cross BBB |
|Tolcapone |COMT inhibitors |Force conversion of |Diarrhea, hepatitic necrosis |Highly metabolized |
|Entacapone |(prevent L-DOPA metabolism to |L-DOPA to DA | | |
| |O-methylated metabolite) |((on-off phenomenon) | | |
|Bromocryptine |D2-agonist & |L-DOPA adjunct |Hallucinations, confusion, nausea,| |
| |partial D1-agonist | |hypotension | |
| | | |Peritoneal fibrosis | |
|Selegiline |MAOB inhibitor |Early PD (delay L-DOPA use) |Nausea, dry mouth, confusion, |MAOA metabolizes 5-HT & NE |
| |(prevents DA metabolism) | |euphoria, insomnia, psychosis |Metabolized to amphetamine |
|Amantidine |DA-releasing agent |Mild PD (short-term) |Dry mouth, confusion, anxiety, |Weak M-antagonist |
| |(blocks uptake into vesicles) |Influenza |anorexia, hallucinations | |
| | | | | |
|General Anesthetics | | | | |
|Methoxyflurane |Inhalation |OB surgery |Sensitizes heart, |Highly metabolized (produces |
| |MOST potent (MAC 0.16%) |Muscle relaxant (except uterus) |renal toxicity (20% mortality) |F-) |
| | |Low-dose analgesia | | |
|Halothane |Inhalation (halogenated alkane) |Anesthesia in kids & asthma |Hypotension, sensitization to |Liver metabolism |
| |High potency (MAC 1atm) |(release of endorphins) |Diffusional anoxia | |
| | |NOT muscle relaxant | | |
|Thiopental |IV |Rapid sequence induction |Injection site necrosis (>2.5% |Rapid redistribution (LOC in |
| |(ultrashort-acting barbiturate) |NOT analgesia |concentration), laryngospasm, |10-20s, recovery in 20-30min) |
| | | |hyperalgesia |(opening of GABAA channels |
|Etomidate |IV |Very short procedures ONLY |Muscle spasms, (cortisol |Recovery in 5min |
| |(ultrashort-acting, | | | |
| |NON-barbiturate sedative) | | | |
|Propofol |IV |Regional (continuous infusion) |Hypotension, (RR, |“milk of anesthesia” |
| |(rapid-acting, |NOT analgesia |allergies (egg products) |(ICP |
| |NON-barbiturate sedative) | |NOT impair renal or hepatic fxn | |
|Ketamine |IV |Marked anesthesia w/ amnesia |Hallucinations, excitement, |Blocks glutamate receptors in |
| |(dissociative anesthetics) |ER, radiology in kids |delirium; preserves respiratory |cortex & limbic system, blocks |
| | |Good analgesia |responses & (CO |( opioid receptors |
|Midazolam |Benzos |Pre-op anxiety & sedation |CNS depression |NOT analgesic |
| |(anesthetic adjunct) |w/ amnesia | |Reverse w/ Flumazenil |
|Fentanyl |Opioids |Cardiac surgery analgesia |N/V, pruritis, respiratory | |
| |(anesthetic adjunct) | |depression (reverse w/ Naloxone) | |
|Succinylcholine |Muscle relaxants |(MAC of inhalation anesthetics |Hyperkalemia, |Depolarizing |
|d-Turbocurarine |(anesthetic adjuncts) | |malignant hyperthermia |NON-depolarizing |
| | | | | |
|Local Anesthetics | | | | |
|Lidocaine |Amides |Anti-arrhythmic |Ventricular fibrillation |Highly protein bound |
| |(oral, parenteral, topical) |Local, regional, epidural, topical| |Hepatic metabolism |
| | | | |Combo w/ vasoconstrictor |
|Bupivacaine |Amides |Epidural or spinal, NOT regional |Hypotension, (contractility, MORE |MORE potent & long-acting |
| | |(parturition & LE orthopedics) |ventricular fib | |
|Ropivacaine |Amides |Epidural or spinal |LESS cardiotoxic |LESS potent |
|Procaine |Esters |LESS potent |Respiratory depression |Shorter acting |
| |(parenteral, NOT topical) | |Allergies | |
|Chloroprocaine |Esters |MORE potent than Procaine | |Rapid metabolism |
|Tetracaine |Esters |Spinal (10X MORE potent) |10X MORE toxic |Slower onset & longer duration |
|Benzocaine |Esters |Topical ONLY | |ALWAYS unionized (lacks amine |
| | | | |group) |
|Cocaine |Local anesthetic & inhibit | |Euphoria, (HR, (RR ( agitation, |NOT combo w/ vasoconstrictors |
| |catecholamine reuptake | |HTN, dyspnea ( seizure, | |
| | | |arrythmias, respiratory failure | |
| | | | | |
|Anti-convulsants | | | | |
|Phenobarbital |Barbiturates |Unclassified seizures |Sedation, cognitive impairment, |Induce P450 |
| |(long-acting) |Status epilepticus |behavioral changes (40% kids), | |
| | | |addiction, rebound seizures | |
|Phenytoin (Dilantin) |Hydantoins |Partial & grand mal seizures |Muscle necrosis, thickened facial |Rate-limited hepatic metabolism|
| | |Status epilepticus (Fosphenytoin) |features, darkened hair, gum |( p-HPPH |
| | | |hypertrophy (esp. kids), |Induce P450 |
| | | |macrocytosis (folate deficiency) | |
|Carbamazepine |Iminostilbenes |Partial & grand mal seizures |Lethargy, ataxia, diplopia, |Slow absorption |
| |((noradrenergic neuron firing & |Mania |neutropenia, aplastic anemia |Similar to TCAs |
| |(SHRFR) | |(rare), hyponatremia (esp. |Induce P450 |
| | | |elderly) | |
|Lamotrigine |Phenyltriazines |Partial & absence seizures |Rash, dizziness, headache, |Metabolism induced by Phenytoin|
| |(blocks Na2+ & Ca2+-channels, |Lennox-Gastaut syndrome |diplopia, ataxia, somnolence |& Carbamazepine, inhibited by |
| |inhibits Glu & Asp release, | | |Valproic acid |
| |blocks photic stimulation) | | | |
|Levetiracetam |(blocks n-type Ca2+-channels) |Partial seizures (esp. w/ comorbid|Somnolence, dizziness, headache |NOT metabolized |
| | |liver dz) | |NO drug interactions |
|Topiramate |Sulfate-substituted fructose |Adjunct for partial seizures |Somnolence, fatigue, impaired |ONLY 20% metabolized |
| |(blocks Na+ & Ca2+-channels, | |concentration, word-finding |Metabolism inhibited by |
| |(GABA binding, inhibits | |difficulties, renal stones, |Phenytoin & Carbamazepine |
| |kainate/AMPA-activated Glu | |paresthesias, weight loss | |
| |receptor) | | | |
|Valproate (Depakote) |Branched-chain COOH |Myoclonic seizures |N/V, (liver enzymes, liver |Rapid absorption |
| |((SHRFR, (GABA binding & |Refractory absence seizures |necrosis (esp. ................
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