Drug List Psych Optho Neuro

Common Name Sub Category Mechanism of Action Clinical Use/Indications Adverse Effects Other

ADHD Meds

Methylphenidate (Ritalin) Increased presynaptic NE vesicular release

Atomoxetine

Clonidine Increase noradrenergic tone in inhibitory synapses

Guanfacine

Buproprion Antidepressants 3rd line for ADHD

Venlafaxine

TCAs Not used in kids because of cardio

Typical Antipsychotic Agents

Chlorpromazine*

Thioridazine*

Mezoridazine

Prochlorperazine

Fluphenazine*

Trifluoperazine*

Haloperidol (Haldol)*

Droperidol

Thithixene

Atypical Antipsychotic Agents

Clozapine*

Olanzapine* Metabolic syndrome

Quetiapine*

Ziptrasidone* No weight gain

Apripiprazole (Abilify)*

Amphetamine-type stimulants

1st line for ADHD - good for attentional symptoms

1. Can be abused and cause psychological and physical dependence

Dexmethylphenidate (Focalin)

Mixed amphetamine salts (Adderall)

Non-amphetamine stimulant

2nd line for ADHD = helps with inattention, overactivity

Alpha-2 Adrenergic Agonist

3rd line for ADHD - helps with hyperactivity, motor symptoms (tics)

Dopamine reuptake inhibitors and dual-reuptake inhibitors (NE/5-HT)

Phenothiazine derivatives

1. Competitively blocking dopamine receptors (D2/D3 ratio = 10-50)2. Inhibit activation of adenyl cyclase and shuts down the mesolimbic system3. D2 receptors located in limbic, extrapyramidal, endocrine structures

1. Treatment of psychosis- Schizo -> positive symptoms- Bipolar- Delirium- Depression w/ psychosis2. Off-label uses- Depression- Aggression- Personality disorders- Eating disorders- Impulse control disorders

Low potency - low incidence of EPS, high sedating/CV effects

High potency - low sedating/CV effects, higher incidence of EPS

Butyrophenone derivatives

Thioxanthene derivative

Serotonin/dopamine antagonists

1. Competitively block serotonin receptors (5-HT2), which inhibits dopamine release in frontal lobes2. Higher degree of binding/blocking D4/D33. Improves negative symptoms of schizo, reduces EPS side effect, improves positive symptoms

See above, except can also treat negative symptoms- Olanzapine for OCD, anxiety, depression, mania, Tourrette's

May cause agranulocytosis

Risperidone (Risperdal)*

Dopamine agonist/antagonist

1. Dop antag in high (mesolimbic) and agonist in low dopamine (frontal lobes)

1. Anticholinergic - dryness2. Extrapyramidal (EPS) - Parkinsonian syndrome - Acute dystornia - spasm of nexk muscles - tx w/ benztropine - Tardive dyskinesia - involuntary movement3. Neuroleptic malignant syndrome (NMS) - blockage of D2 in hypothalamus - hyperthermia, hypertension, dyskinesia - tx w/ dantrolene/bromocriptine4. Sedation5. Cardiovascular - prolonged QT, ECG change6. Endocrine --> galactorrhea, amenorrhea

Atypicals have better side effect profiles


Mood Stabilizers

Lithium* Classic 1. Possibly inhibits phosphoinositol cascade

Lamotrigine Anticonvulsants Interferes w. Na channels and reduces excitation

Carbamazepine Acts on Na/K channels to enhance GABA Only use if Lithium or Valproic acid fail

Oxcarbazepine Similar to Carbamazepine, with better side effects

Gabapentin

Symbyax

Antipsychotics

Benzodiazepines

Antitussives and Mucokinetic Agents (Coughing)

Codeine

Hydrocodone

Dextromethorphan

Promethazine/phenerga

NOT 1st line antitussive

Benzonatate

GI tract issues

N-Acetylcysteine

Demulcents Sticky substances that protect lining of resp tract

1. 1st line for acute bipolar depression - prophylaxes depression2. Blocks relapse and acute manic events

1. LMNOP - Lithium- Movement (tremor)- Nephrogenic DI- hypOthyroidism- Pregnancy problems 2. Need to monitor closely - toxicity seen at 1.5-2 mEq/L

Drug interact:↑ - DAMN (Dehydrate, AceI, Metro, NSAID)↓ - COAST (CA inhib, Osmotic, Antacid, Salt, Caffeine)

1. Prophylax depression - Bipolar depression (treatment and maintenance)

1. Dizziness, sedation, diplopia, ataxia2. Pregnancy issue3. Severe rash/Steven Johnson syndrom

Valproic Acid (Depakote)

Interferes w/ Ca/Na channels, enhances GABA, inhibits glutamate

1. Acute mania and in rapid cycling bipolar/mixed episodes

1. Pregnancy Issue (D)2. Sedation, dizziness3. Can induce Hepatitis/hepatic fail, pancreatitis, abnormal bleeding

Drug interact - ↑ - aspirin, felbamate↓ - Rifampin

1. Pregnancy Issue (D) - spina bifida2. GI, dizziness, Agranulocytosis4. Hepatitis/cholestatic jaundice5. Steven Johnson

Induces own metabolism - watch hepatic enzyme - Be careful of asians

Other mood stabilizers

Centrally acting antitussives (anodynes)

1. Non-specifically reduce excitability of cough center

1. Non-productive cough - when cough results in sleep loss- to prevent herniation, spread of infection

1. Resp depression - caution in < 22. Constipation, miosis, sedate, addict

Opioids - doses < for cough vs analgesia

Fewer side effects- Confusion, excitation, nervous, resp depression in high dose - high abusive potential

Non-opioid - d-isomer of codeine- don't use with MAOIs

Diphenhydramine (Benadryl)

Peripheral acting antitussive

Reduce afferent inputs to the cough center - on stretch receptors in the respiratory passage

1. Can cause hypersensitivity rxn - procain/tetracaine2. DON'T CHEW - anesthesia

Guaifenesin - Robitussin/Humibid

Mucokinetic - Expectorants

Stimulate/modify mucous production in bronchi - stomach irritant that causes bronchial secretion

1. Productive coughs- Expectorants - thick/tenacious cough secretions- Mucolytics - cystic fibrosis, antidote to acetaminophen poisoning

Mucokinetic - Mucolytics

Break down sputum aggregates to smaller parts - splits disulfide bonds - Nebulize

Smells bad, tastes horrible

Mucokinetic - Demulcents


Anti-Emetics (vomiting)

Chlorpromazine Antipsych Pentothiazine derivatives

Prochlorperzine

Promethazine

Thiethylperazine

Droperidol Butyro derivative

Scopolamine Anticholinergic Motion sickness Derm patch

Diphenhydramine Blocks Ach receptors in vest nuclei and CTZ Motion sickness Sedation, blurred vision, dry mouth aka Benadryl

Dimenhydrinate aka Dramamine

Hydroxyzine Vertigo, motion sickness 1. Pregnancy issue

Meclizine

1. Contraindicate in children

Ondansetron

Granisetron

Dolasetron

Polonosetron

Trimethobenzamide 1. Post-op n/v and coughing

Metoclopramide

Dronabinol Vestibular Impairs cognitive and motor fx

Aprepitant Potent CYP3A4 inhibitor

Sedative-Hypnotic Drugs

Aplprazolam

Triazolam*

Lorazepam*

Oxazepam

Flurazepam

Prazepam

Diazepam*

Pehnobarbital

Mephobarbital

Pentobarbital

Secobarbital

Thiopental

Chloral hydrate Historical Hepatic injury

1. Depresses excitability of the CTZ by blocking D2 receptors and transmission2. Also peripherally blocks D2 in GI

1. Radiation/drug induced vomiting 2. Thiethylperazine used for post-op3. Doperidol has tranquilizing effects

1. Sedation2. EPS3. Allergic

Blocks Ach receptors in CTZ, vest nuclei and GI tract

Sedation, blurred vision, reduced GI/bladder tone

Antihistamines - Ethanolamine

Antihistamine- 1st gen pipera

Promethazine (phenergan)

Antihistamine - phenothiazine

Also binds H1 histamine receptors

Serotonin blockers

Selectively blocks serotonin receptors (5-HT3) in GI and CTZ

1. Post-op n/v following highly emetogenic surgery2. drug-induced n/v (antineoplastics)3. Radiation therapy n/v4. NO motion sickness

1. No EPS2. Headache, diarrhea, constipation, phlebitis

Benzamide derivatives

Antiemetic - depresses CTZ (D2)Antitussive - suppresses laryngeal reflex

1. CNS depression2. EPS, Reye's syndrome

1. Prokinetic 2. Anti-emetic - antagonism of dopamine

1. GE reflux2. Daibetic gastric stasis3. N/v assoc w/ cisplatin, radiation

1. CNS depression2. EPS

Other - nausea vomiting

N/v due to antineoplasticsAnorexia w/ weight loss in AIDS

Benzodiazepeines (short acting)

1. Binds to site on GABA A receptor, which enhances GABA's effect2. Mediates both sedation and memory effects 3. Benzo + GABA = increased freq of channel-opening events (Cl-)

1. Anxiety2. Spasticity3. Status epilepticus (lorazepam, diazepam)4. Detox5. Night terrors, sleepwalking6. Insomnia (estazolam, fluraz, quaz, tema, triazolem) - bind 3 alpha-1 sybtype

1. Potential abuse - lethal:effective dose = 200:12. Withdrawal3. Daytime drowsiness 4. Respiratory impairment

1. Antacids decrease absorp2. Antihist/barbit/ETOH increase depression3. CYP450 except loraz, oxaze, temaz

Benzodiazepeines (long acting)

Barbiturate Sedative-hypnotics

1. Barbiturates + GABA = increased duration of channel-opening events (Cl-) -> decreased neuron firing

1. Anticonvulsant - seizures2. Basal anesthesia 3. Narco-analysis4. Decreases respiration - neurogenic/chemical/hypoxic drives

1. Contraindicate in porphyria2. Dependence 3. Lethal, especially with alcohol

Lots of interactions because of P450


Antihistamines Sedating antihistamine 25-50 mg hs

Trazodone Antidepressan

Ramelteon

Zolpidem (Ambien) Insomnia

Zaleplon (Sonata)

Eszopiclone (Lunesta)

Antidepressants

Fluoxetine (Prozac)

Sertraline (Zoloft) Shorter half life, better

Paroxetine (Paxil)

Citalopram (Celexa)

Escitalopram (Lexapro)

Fluvoxamine

Imipramine

Desipramine

Amitripltyline

Nortriptyline

Venlafaxine (Effexor) Similar to SSRIs

Duloxetine

Phenelzine MAO inhibitors

Tranylcypromine

Blocks reuptake of norep and dop

Mirtazapine Noradrenaline + serotonin (NaSSA)

Nefazodone Serotonin antag reuptake inhibitors (SARI)

Trazodone

Diphenhydramine (Benadryl)

Melatonin agonist

Imidazopyridine derivative

Act on alpha subunit of GABA A - selectively bind to receptor to produce hypnotic effects

Rapid acting, short half-life

Pyrazolopyrimidine class

Useful for middle of night insomnia

Selective Serotonin Reuptake Inhibitors (SSRIs)

1. Selectively block uptake of serotonin2. Advantages - more benign than TCAs, no quinidine action on heart, no significant weight gain3. High safety margin

1. Depression2. OCD, panic disorders, PRSD3. Eating disorders, GAD4. PMS

1. Transient - nervousness, insomnia, nausea, diarrhea2. Persistent - sexual dysfx3. Serotonin syndrome - confusion, fever, altered consciousness, myoclonus4. Inhibits p450

Takes a long time to reach steady state

More sedating, better for anxiety

Tricyclic antidepressants (TCA)

1. Block active reuptake of norep and serotonin - higher levels in synaptic cleft2. Original gold standard

1. Resistant depression 2. Enuresis in childhood (Imipramine)3. Chronic pain, neuralgias, miagraine, diabetic neuropathy

1. Sedation, anticholinergic2. ECG change3. Weight gain, impotence4. Can precipitate mania

If overdosed (cardiac monitoring) use gastric lavage, NaHCO3, Lidocaine or Phenytoin

Serotonin + Norep reuptake inhibitors (SNRI)

Reuptake inhibitor of serotonin, norep, and some dopamine

1. Depression, GAD, Panic2. PTSD, PMS

1. Liver metabolized2. Dose dependent HTN

Less risk of liver issue, can treat Diabetic neuropathy

Inhibits MAO A and B non-selectively, which result in higher norep and serotonin release

1. Better for bipolar/atypical depression2. Phobias3. Migraines4. Neurodermatitis

1. Weight gain, sexual dysfx2. Hepatotoxic3. Slower onset

1. Tyramine food, amphetamines -> HTN crisis

Sexual dysfunction Faster onset

Buproprion (Wellbutrin, Zyban)

Norep + dopamine reuptake inhib (NDRI)

1. Depression (fewer sex side effects)2. Smoking cessation - Zyban3. ADHD

1. Agitation, insomnia, seizures2. Inhibits 2D6


General Anesthetics

Nitrous Oxide (N2O) Gases Nonvolatile

Halothane

Enflurane

Isoflurane

Desflurane

Sevoflurane

Ketamine IV agents

Propofol

Etomidate Minimal CV effects

Local Anesthetics

Bupivacaine Amides Long acting

Ropivacaine

Lidocaine Medium Acting

Tetracaine Esters Long duration

Cocaine Medium + surface

Procaine Short duration

Benzocaine Surface

Intraocular Pressure (IOP) Lowering Agents - Ocular Hypertensives

Brimonidine Alpha agonists Activates alpha 2 - inhibits aqueous secretion dry mouth, hypotension, lethargy Don't use in kids

Timolol Beta blockers Blocks beta receptors - decrease aqueous secre Bradycardia, bronchospasms, fatigue, worse myasthenia gravis

Inhibits CA, which decreases aqueous production

Acetazolamide

Mannitol CHF, urinary retention, back acne, MI

Glycerin vomiting, less CHF, similar to mannitol

Isosorbide same as glycerin, but safer in DM

Pilocarpine Miotics

Echothiophate iodide Indirect - blocks Ach-esterase Retinal detachment, myopia, angle closure

Latanoprost Prostaglandins F2 - increase matrix turnover = increased flow Increase melanin, blurred vision, URI symptoms, myalgia

Dipivefrin

CNS depressants- ↓ blood soluble = rapid induction/recovery- ↑ lipid soluble = ↑ potency = 1/MAC- ↑ ventilation + concentration = more rapid uptake

Must combine w. IV narcotics, barbiturate and relaxants

1. Bone marrow suppression in high conc2. Neuropathy

1. Massive hepatic necrosis (halothane hepatitis) in 1/35,000, less in children2. slows HR, decreases MAP/CO

1. Depressed heart contractility2. Decreased smooth muscle tone, PVR, TV3. Blocks vent response to hypoxia

1. Free F- released = renal fail (preexist)2. Increases HR, decreases MAP/CO

1. No renal dysfx, minimal metab2. Increases HR, decreases MAP/CO + SVR

1. Minimal liver biotransform2. Increases HR, decreases MAP

1. Same as enflurane - disolve in soda lime2. Little heart effect

Muscarinic receptor antagonistOpiate receptor agonistProduces dissociated anethesia

1. Myocardial depressant2. Depresses respiration

More rapid recovery than barbiturates

1. Blocks voltage dependent Na channels - block AP2. Absorption - short = limited, need vasoconstrictor3. Vasodilate except for cocaine4. Esters metab by pseudocholinesterases, Amides by hepatic microsomal enzymes

1. Minor surgery2. Spinal anesthesia3. Regional anesthesia4. Infiltration anesthesia5. Post-op analgesia

1. CNS - lightheaded, restless, tonic-clonic2. CV - cocaine = htn, mi, cerebral hemorrhage3. Allergy - esters4. Treat convulsions w/ diazepam or barbiturates

1. Open angle glaucoma2. Ocular hypertension

Dorzolamide hydrochloride

Carbonic Anhydrase Inhibitors

Drops - bitter taste, diuresis, fatigue, Stevens-Johnson

Don't use w/ sulfa allergy, hyponatremia/kalemia, thiazides or digitalis

Oral/IV - hypokalemia, renal stones, aplastic anemia, Stevens-Johnson

Hyperosmolar agents

Dehydrates vitreous and draw fluid into intravascular space

Direct - stimulate muscarinic receptors to cause constriction and increase flow

Angle closure, breakdown of barrier, retinal tears - don't use in young patients

Sympathomimetic

Beta stimulation in trabecular network = increased flow

Cystoid macular edema, mydriasis, blurred vision, tachycardia, htn, headache


Other Eye Drugs

Penicillin, etc Antibacterials Self-explanatory

Tropicamide Dilating drops Eye drops Mydriasis and cycloplegia (paralysis)

Atropine sulfate

Phenylephrine Sympathomimetic - stimular dilator muscle

Macugen Anti-VEGF

Lucentis Recombinant fragment that ragets VEGF-A

Avastin Parent of Lucentis

Migraine Drugs

Acetaminophen Analgesic Ideal for pregnant - contra in severe kidney/liver disease, G6PD

Aspirin NSAIDs

Naproxen

Isometheptene (Midrin) Combine to prevent migraine

Metoclopramide Good for nausea and vomiting

Sumatriptan Triptans

Zolmitriptan Oral, nasal - liver

Naratriptan Oral - renal

Rizatriptan Oral- no renal/liver

Almotriptan Oral - liver

Frovatriptan Oral - renal

Eletriptan Oral - liver

Ergaotamine Ergot alkaloids Oral - only 2x/wk

Dihydroergatamine IV/nasal - avoid preg

Chlorpromazine Neuroleptics Prolonged migraine + signif n/v

Opioids Don't respond to normal tx Safe for pregnant when limited

Propranolol Beta blockers Without sympathomimetic activity Migraine prevention

Timolol

Divalproex Anti-epileptic GABA agonists Pregnancy group D, liver issues

Topiramate

Verapamil Ca blockers Significant cardiac (Class 4 antiarrhy)

Flunarizine Not in US

TCAs Antidepressants

Non-steroidals/Corticosteroids

Antiinflammatory

Parasympatholytic - block Ach receptors in iris ciliary body - mydriasis and cycloplegia

Pegylated oligonucleotide binds to VEGF 165 and prevents ability to bind to receptor

Stops angiogenesis/neovascular in:1. macular degen (wet), DM retino2. Neovascular glaucoma, retinal vein occlusion

1. Blurred vision, pain, redness of eye, increased IOP, retinal detachment2. Dizziness, headache, nausea, diarrhea3. Beware hypersensitivity rxn

Mild-moderate migrainesJust helps with the pain

1. 5-HT1B/D agonists, some 1F (1B = bv, 1D/F = neurons)2. Selectively constrict cranial vessels and reduce inflammation3. Block pain transmission from CN V to trigeminal nucleus caudalis4. All except sumatriptan are more centrally penetrant

Abort Moderate-Severe migrainesIf doesn't abort in 2-4 then medication won't help

1. Contraindications - Heart disease/MI- Angina, HTN- basilar migraine2. Triptans can't be used w/ other triptans or ergot or MAOIs3. Too much ergot = poisoning

Oral, subQ, nasal - liver/renal

1. 5-HT1B/D agonists2. Additional receptor affinities

1. Decreased sexual activity, bradycardia, lethargy

High efficacy, mild/moderate adverse effects

Severe cardiac effects, orthostatic hypotension


Parkinson's Drugs - Dopamine agents

Levodopa Levodopa

Trihexyphenidyl Anticholinergic Blocks central muscarinic receptors Mild tx for Parkinson's - tremor + rigidity

Benztropine

Bromocriptine Stimulate dopamine receptor directly Ergot derivatives

Pergolide

Pramipexole

Ropinirole

Apomorphine

Entacapone Inhibit breakdown of dopamine by COMT Adjunct w/ L-dopa - increases ON time Orange discoloration of urine, diarrhea

Tolcapone Fatal hepatitis

Selegiline Inhibit breakdown of dopamine by MAO Serotonin syndrome w/ SSRIs

Rasagiline

Amantadine Other Dopaminergic, anticholinergic, NMDA antag Mild tx - tremor, rigid, bradykinesia Peripheral edema, hallucinations

Antipsychotics

Reserpine

Tetrabenazine

Botulinum toxin Poison Inhibits release of Ach at the NMJ

Antiepileptic drugs

Benzodiazepines - GABA-A - Cl channel opens more Tx of choice for acute seizures Sedation, resp depression Lorazepam/Diazepam

Barbiturates GABA-A - Cl channel opens longer Refractory status epilepticus bad side effects- only use in infant, poor Phenobarbitol (IV)

Tiagabine Selective GABA reuptake inhibitor Partial seizures Can cause absence epilepticus, sedation

Phenytoin Voltage/Frequency dependent block of Na channel Partial and GTC seizures Nonlinear pharmaco

Carbamazepine SJ syndrome, asians

Oxcarbazepine Not as bad

Lamotrigine Enhances the slow inactivated state of channel Good for all seizures Headache, insomnia, rash Good for Preg women

Lacosamide Enhances slow inactivation of the channel New drug

Ethosuximide Only absence seizures

Valproate Multiple MOAs 1. ↑ synaptic GABA, 2. ↓ NMDA excite Good for all seizures

Topiramate 1. ↑ Cl events, 2. ↓ glutamate, Ca channels All except absence seizures Very safe - paresthesias, cog impair, weight loss

Zonisamide 1. Na channels, 2. Ca channels, 3. CA inhib Good for all seizures Typical side effects, decreased appetite

Levetiracetam Unique MOAs Binds vesicle protein SV2A - unknown Good for all seizures Safe - sedation, irritability Works fast

Gabapentin/Pregabalin a2 subunit of Ca channels Partial seizures - pain Mild - sedation, weight gain Short half-life

Dopamine replacement - absorbed in SB through LNAA - converted to dopamine + O-methyl dopa by DDC

Most effective for treating Parkinson's - tremor, rigidity, bradykinesia

Nausea, hypotension, hallucinations - Must be administered w/ carbidopa, a DDC inhibitor

dry mouth, sedation, blurry vision, urinary retention

Dopamine agonist

Moderate tx for Parkinson's - tremor, rigidity, bradykinesia

PUD, vasoconstrictive, pulm fibrosis, hallucination, valve disease (pergolide)

Somnolence, leg edema, compulsive behavior

Nonergot derivative w/ specificity for the D3 receptor

COMT inhibitors

MAO-B Inhibitors

Mild tx - tremor, rigid, bradykinesia, potentially neuroprotective

Non-selective MAO I's = tyrosine effect

Dopamine Receptor Blockers and Depleters

Focal dystonia - cervical dystonia, blepharospasm, hemifacial spasm

Lasts 3-6 months - could overweaken muscles

GABA affecting

Na channel effecting

Thrombophlebitis, sedation, dizziness, diplopia, hepatotoxicity, myelosuppression

Ca channel affecting

Blocks T-type Ca channels in thalamus - stops abnormal thalamic excitability

Sedation, dizziness, headache, behavioral, myelosuppression

Cog impairment, weight gain, hair loss, tremor, bad for pregnant

Hepatic failure, polycystic ovary

B193

Luke:


Drugs of Abuse and Addiction

Alcohol Metabolized via dehydrogenase system

Heroin/Morphine Opioids Binds to mu receptors CNS/resp depression, miosis Tx: ABCs, Narcan for acute, supportive

Barbiturates

Benzodiazepines

Chloral hydrate

GHB

Cocaine Stimulants

Ecstasy Euphoria, hallucin, tense jaw, bruxism

LSD Hallucinogens Interacts with serotonin receptors Euphoria, panic attacks, paranoia Treatment - supportive

Phencyclidine (PCP) Related to ketamine - CNS depressant Tachy, htn, ataxia, seizure, coma

Marijuana drowsiness, euphora, paranoia

Hydrocarbons Inhalants CNS depressants Euphoria, dysrythmias, met acid Chronic: met acidosis, hypokal

Nitrous Oxide (N2O) transient euphoria, CNS depress Chronic: polyneuro, mega anemia

Paregoric

Morphine Analgesic, dyspnea due to PE

Codeine Mild/moderate pain, antitussive

Heroin Schedule 1, 3x more than morphine

Apomorphine Parkinsons

Oxycodone oral analgesic

Hydromorphone moderate/severe pain Dilaudid - good renal

Meperidine Not antitussive, local anesthetic

Fentanyl Post-op/chronic pain, anesthesia

Diphenoxylate Diarrhea

Loperamide acute, non-specific diarrhea

Methadone mod/severe pain, opioid dependency

Darvocet No clinical usefulness

Pentazocine Moderate pain due to kappa receptor Schedule IV drugs

Nalbuphine

Naloxone Antagonize opioid effects Need to assist resp depression w/ vent

Naltrexone Treat opioid dep, alcohol, detox Liver toxicity

Buprenorphine Partial agonist Mu Agonist to a ceiling, submaximal response Prevent opioid withdrawal, so good for opioid dependence

PAMOR antagonists Analgesic effect

Binds GABA, dilates bvs, decreases glutamate, reduces ADH secretion

Wenicke, Korsakoff, cirrhosis, PUD, fetal alcohol syndrome, pancreatitis - BAD w/ acetaminophen

Tx: supply thiamine, benzos, disulfiram

Sedative-hypnotics

1. Enhance GABA2. GHB - odorless, colorless3. Chloral hydrate - pear-like odor

1. CNS/resp depression, lethargy, coma2. GHB - agitation, seizure, brady, amnesia3. Chloral - dysrthmias4. Withdrawal - insomnia, n/v, sweat, tachy

Treatment:1. Supportive care2. Phenobarb - urine alkalinization3. Chloral - beta blokcers4. Benz - Flumazenil

1. Block presynaptic reuptake of dopa, norep, serotonin2. Produces vasoconstrict and local anesthetic

1. ↑ HR/BP, euphoria, strokes, rhabdomyolysis, seizures, renal fail

Treatment: supportiveHyperthermia - ice, Seizures - Benzo, phenobarbHTN - sodium nitroprusside, phentolamine

Tx: supportive, beta-blockers for dysryth

Naturally occuring opioid agonist

1. Inhibit firing of neurons in dorsal horn, limbic structures and cerebral cortex2. ↓ adenylyl cyclase -> ↓ cAMP -> ↓ Ca influx or ↑ K efflux -> ↓ neurotransmitter release3. Targets mu receptors

Treats diarrhea/intestinal colicNeonatal opioid dependency

1. Seizures (Meperidine)2. Depress resp 3. Emetic effect - n/v4. Miosis (morphine)5. Antitussive - lower dose than analgesic6. Bowel dysfx/constipation7. CV - hypotension/brady8. Euphoria, sedation9. Dependence

Semi-synthetic agonist

Synthetic agonists

agonist/antagonist

Agonists at kappa receptor, antagonists at mu receptor

Potential abuse, psychotomimetic, hallucinatory and dysphoric effects

Pure antagonists

Binds all opioid receptors with higher affinity than agonist and reverse effects of agonists

Alvimopan/Methynaltrexone

Restricted antagonists

Reduction in bowel dysfunction, constipation

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Drug List Psych Optho Neuro