Date post: | 26-Oct-2014 |
Category: |
Documents |
Upload: | ashley-barrile |
View: | 50 times |
Download: | 0 times |
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
Common Name Sub Category Mechanism of Action Clinical Use/Indications Adverse Effects Other
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
Common Name Sub Category Mechanism of Action Clinical Use/Indications Adverse Effects Other
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
Common Name Sub Category Mechanism of Action Clinical Use/Indications Adverse Effects Other
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
Common Name Sub Category Mechanism of Action Clinical Use/Indications Adverse Effects Other
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
Common Name Sub Category Mechanism of Action Clinical Use/Indications Adverse Effects Other
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
Common Name Sub Category Mechanism of Action Clinical Use/Indications Adverse Effects Other
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
Common Name Sub Category Mechanism of Action Clinical Use/Indications Adverse Effects Other
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