Neuropharm-Final

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Local Anesthetics (Amides)

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lidocaine, bupivacaine, mepivacaine, ropivacaine. metabolized in liver

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local anesthetics (esters)

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proxaine, benzocaine. prone to allergic rxns. metabolized quickly by pseudocholinesterases in serum.

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procaine

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ester local anesthetic. use if amide c/i (liver tox)

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benzocaine

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ester local anesthetic. very hydrophobic. found in OTC teething gels. weak, topical, local rxn only

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local anesthetic MOA

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MOA: block Na Channels, decr AP. Speed of onset due to pKa and tissue pH. Necrotic tissue has decr pH, so hard to numb

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local anesthetic tox

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proportional to lipid solubility. AE: cardiotox, arrhythmias, death if systemic absorp. use epi to prolong duration and limit tox

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IV general anesthetics

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thiopental, propofol, ketamine, fentanyl

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thiopental

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barbituate for IV general anesthetic. Rapid MOA

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ketamine

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NMDA-R blocker, IV general anesthetic. Dissociative anesthesia

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fentenyl

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opiate, short acting, good IV general anesthetic or patch (chronic pain). for heroin withdrawal

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propofol

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IV gen anesthesia. similar to barbiutate. used in same-day discharges (fast recovery)

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IV general anesthetics danger

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malignant hyperthermia due to incr myoplasmic ca. Give dantrolene

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Inhaled general anesthetics

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NO, halothane

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inhaled gen anesthetic MOA

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enhance GABA

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MAC

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median alveolar conc. important in inhaled gen anesthetics. amount to affect 50% of pop. NO has high MAC (not used alone). More lipid sol = low MAC

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opioids use, MOA, and tox

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for pain, diarrhea, coughs. Mu (analgesia), Kappa (dorsal horn), Delta receptors. AE: itching, small pupils, sedation, nausea

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opioid strong agonists

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morphine, meperidine, oxycodone (short term), fentenyl, methadone, heroine

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morphine

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IV opiate due to 1st pass metab. strong agonist.

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methadone

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oral opiate. strong agonist. mild withdrawal. for severe pain and heroin withdrawal

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meperidine

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synthetic strong agonist opiate. for labor. no AE of seizures

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heroine

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IV opiate. exaggerated euphoria

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opioid medium agonists

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codeine (less potent, for mod pain and cough suppressent), hydrocodone (for mod pain. less potent than morphine)

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opioid weak agonist

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tramadol (little addiction)

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opioid mixed receptor

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buprenorphine (for opiate dependence)

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opioid antagonist

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naltrexone (for chronic alcoholism), naloxone (reverse coma and resp failure due to opioid OD)

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opioid withdrawal

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stage 1, stage 2, stage 3. Stage 3: 3 days: tachy, chills, seizure, musc spasm.

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aspirin AE

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Reye's syndrome.

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3 NSAIDs as second line

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indomethacin, sulindac, phenylbutazone

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barbitol, thiopental

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barbituate anxiolytics. barbitol: epilepsy, thiopental: anesthesia. Bind to GABAa. no longer used

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benzodiazepines AE and C/I

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sedation, rep failure (at high dose), addiction, withdrawal sx. C/I: liver dz, glaucoma, alcohol

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long acting benzodiazepine

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clonazepam. 1 day half life. for epilepsy, sleep, anxiety

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medium acting benzodiazepines

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alprazolam (xanax), drazepam (valum), lorazepam (ativan), tomazepam (restoril)

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benzodiazepine antagonist

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flumazenil: GABA-R antagonist for fast benzo reversal. 1 hr half-life

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buspirone

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for generalized anxiety. slower than benzo. MOA: 5HT1a-R. low AE/dependence

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zolpidem (ambien), zaleplone (sonata), eszopiclone (lunesta)

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hypnotics. Act on benzo-R. not additive, no rebound insomnia

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mood stabilizer (bipolar) drugs

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Anticonvulsants: carbamazepine, valproic acid, lamotrigine; Lithium (proph +acute)

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lithium

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for proph and acute manic episodes. oral. renal excr. low therap index. many AE. no effect seen in nl ppl

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anticonvulsants/epileptic drugs and AE

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phenobarbital, phenytoin, carbamazepine, valproic acid, ethosuximide. bone marrow suppression (CBC), teratogenic, osteopenia (give Ca), hepatotox(LFTs), hypersens rash (S-J syndrome)

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phenobarbital

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anticonvulsant/epileptic. block Na channels. Induce p450. most sedating/cog impairement. For neonatal seizures, status epilepticus

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phenytoin

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blocks Na. induce p450. widespread seizure use. AE gingival hyperplasia

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carbamazepine

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Na blocker. Induce p450. for partial complex seizures, bipolar, trigeminal neuralgias

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valproic acid

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Na blocker, and incr brain GABA. p450 inhibitor. for generalized epilepsy, bipolar, migraine. worst teratogen (no <5yo). AE fat

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ethosuximide

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anticonvulsant/epileptic. blocks T-type Ca channels. for absence epilepsy

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leviteracetum, gabapentin

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anticonvulsant/epileptic. excreted unmetab through kidney (for liver dz pt). gabapentin for neuropathic pain

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lamotrigine

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anticonvulsant for bipolar (like valproic acid, carbamazepine)

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topiramate

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anticonvulsant. prevents migraine. weight loss. AE cog impairment

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TCA

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antidepressants. amitriptyline, imiprimine. block reuptake of NE and 5HT. AE dry mouth, constipation, urinary retension, blurred vision, arrhythmia

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amitryptiline

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TCA. for chronic pain, migraine, depression

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imipramine

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TCA. for bed wetting, depression

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SSRI

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fluoxetine, citalopram, sertraline, paroxetine. inhibit 5HT reuptake. AE sedation, N, DDI, insomnia

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fluoxetine

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prototypical SSRI. depression, anxiety

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citalopram

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SSRI. like fluoxetine, but also chronic pain, HA

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sertaline

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SSRI. like fluoxetine, but less cog impact

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paroxetine

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SSRI. like fluoxetine, but wt gain

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SNRI

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venlafaxine. block reuptake of NE and 5HT. For depression, anxiety, HA, neuropathic pain. less wt gain, better efficacy

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atypical antidepressants

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buproprion, trazodone

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buproprion

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atypical. blocks reuptake of NE and dopa. (no serotonin syndrome?). Depression, NOT anxiety. no wt gain, sedation, sex dysfunction. SEIZURES

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trazadone

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atypical. blocks post synaptic 5HT-R. VERY sedating. for depressed insomniacs. can cause priaprism

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tranycypramine, phenelzine

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MAOI. inhibit breakdown of NE and 5HT. effective. limited indications. only for extreme refractory depression. AE HTN Crisis

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Hypertension crisis

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tyramine poisoning. monoamine metabo in gut is blocked by MAOI. --> NE incr

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serotonin syndrome

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incr serotonin --> cog, autonomic, somatic effects. antidepressants

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caffeine

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adenosine receptor antagonist (incr intracell cAMP)

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nicotine

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nicotinic agonist. affects locus ceruleus (NE) and limbic reward system

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cocaine

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blocks monoamine reuptake transport. Na channel blocker

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methamphetamine

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blocks reuptake of dopamine

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MDMA (ecstasy)

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release of serotonin, dopa, NE. time/perception distorting, sex enhancer

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PCP (angel dust)

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hallucinogen, blocks NMDA glutamate receptors

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THC

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cannabinoid-R agonist

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levodopa + carbidopa

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gold standard Parkinson's. AE: psychosis, N/V, dyskinesias(w chronic use)

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bromocriptine, pramipexol

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dopamine agonists for PD

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selegiline

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MAO B inhibition (prevents dopa breakdown) for PD

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amantidine

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incr release of dopa for PD

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trihexyphenidyl

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anticholinergic (for PD)

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Parkinson's gold standard

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levodopa + carbidopa. AE: psychosis, N/V, dyskinesias (with chronic use)

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Parkinson drugs

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*levodopa + carbidopa; bromocriptine; pramipexol; selegiline; amantidine; trihexyphenidyl

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typical anti-psychotics

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chloropromazine, haloperidol. D2 antagonists. AE: EPS, serum prolactin, tardive dyskinesia with chronic use

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atypical anti-psychotics

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risepridone, clozapine, olanzapine. 5HT2A/D2 antag. AE: no EPS, prolactin, tardive dyskinesia, BUT agranulocytosis

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extra-pyramidal symptoms (EPS)

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with typical antipsych drugs. dystonic rxn, Parkinsonism, akathia (internal motor), tardive dyskinesia. treat w anticholinergics. neuraleptic malignant syndrome

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prevent migraines

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beta blockers, amitriptyline (TCA), verapamil (Ca-channel blocker)

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sumatriptan

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triptan. for migraines. 5HT1D agonist. subcu, intranasal, oral. AE: MI!!!

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DHE

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ergot for migraines. 5HT1D agonist. IV only. C/I preg, CAD/periph vasc dz. AE: nausea

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migraine drug action

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5HT1D agonists. vasoconstriction or inhibit proinglamm neuropeptides

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alzheimer's drugs

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donepazil/rivastigmine (Ach-ase inhibitors); memantine (blocks some NMDA-R). Affect basal nucleus of Maynert

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succinylcholine

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for surgical paralysis. depolarizing neuromuscular blocker. short acting/rapid for emergent intubation Irreversible w/ drugs! initial phase: fasiculation, then refractory

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succinylcholine AE

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RARE, but bad. hyperkalemia, prolonged paralysis, malignant hyperthermia

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vecuronium, rocuronium, pancurinium.

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for surgical paralysis. non-depol NMJ blocker/comp. inhibit Ach. lasts long. pharm reversed with neostigmine

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edrophonium

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IV periph cholinesterase inhibitor. short onset and duration. for tensilon test of myasthenia gravis

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pyridostigmine

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oral periph cholinesterase inhibitor. for myasthenia gravis

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neostigmine

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periph cholinesterase inhibitor. To reverse surgical paralysis (due to non-depol NMJ blockers)