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Sub Category
Clinical Use/Indications ADHD Meds 1st line for ADHD - good for attentional symptoms
Adverse Effects 1. Can be abused and cause psychological and physical dependence
Methylphenidate (Ritalin) Amphetaminetype stimulants Dexmethylphenidate (Focalin) Mixed amphetamine salts (Adderall) Atomoxetine Nonamphetamine stimulant Clonidine Alpha-2 Adrenergic Guanfacine Agonist
2nd line for ADHD = helps with inattention, overactivity Increase noradrenergic tone in inhibitory synapses 3rd line for ADHD - helps with hyperactivity, motor symptoms (tics)
Typical Antipsychotic Agents Chlorpromazine* Thioridazine* Mezoridazine Prochlorperazine Fluphenazine* Trifluoperazine* Haloperidol (Haldol)* Droperidol Thithixene Butyrophenone derivatives Thioxanthene derivative Phenothiazine derivatives 1. Competitively blocking dopamine receptors (D2/D3 ratio = 10-50) 2. Inhibit activation of adenyl cyclase and shuts down the mesolimbic system 3. D2 receptors located in limbic, extrapyramidal, endocrine structures 1. Treatment of psychosis - Schizo -> positive symptoms - Bipolar - Delirium - Depression w/ psychosis 2. Off-label uses - Depression - Aggression - Personality disorders - Eating disorders - Impulse control disorders 1. Anticholinergic - dryness 2. Extrapyramidal (EPS) - Parkinsonian syndrome - Acute dystornia - spasm of nexk muscles - tx w/ benztropine - Tardive dyskinesia - involuntary movement 3. Neuroleptic malignant syndrome (NMS) - blockage of D2 in hypothalamus - hyperthermia, hypertension, dyskinesia - tx w/ dantrolene/bromocriptine 4. Sedation 5. Cardiovascular - prolonged QT, ECG change 6. Endocrine --> galactorrhea, amenorrhea Atypicals have better side effect profiles
Atypical Antipsychotic Agents Serotonin/dopa 1. Competitively block serotonin receptors (5mine HT2), which inhibits dopamine release in frontal lobes Risperidone (Risperdal)* antagonists 2. Higher degree of binding/blocking D4/D3 3. Improves negative symptoms of schizo, reduces Olanzapine* EPS side effect, improves positive symptoms Quetiapine* Clozapine* Ziptrasidone* 1. Dop antag in high (mesolimbic) and agonist in Apripiprazole (Abilify)* Dopamine agonist/antagoni low dopamine (frontal lobes) st See above, except can also treat negative symptoms - Olanzapine for OCD, anxiety, depression, mania, Tourrette's
Common Name
Sub Category
Mechanism of Action
Adverse Effects
Lithium*
Classic
1. 1st line for acute bipolar depression prophylaxes depression 2. Blocks relapse and acute manic events
Lamotrigine
1. Prophylax depression - Bipolar depression (treatment and maintenance) 1. Acute mania and in rapid cycling bipolar/mixed episodes
Carbamazepine
1. LMNOP - Lithium - Movement (tremor) - Nephrogenic DI - hypOthyroidism - Pregnancy problems 2. Need to monitor closely - toxicity seen at 1.5-2 mEq/L 1. Dizziness, sedation, diplopia, ataxia 2. Pregnancy issue 3. Severe rash/Steven Johnson syndrom 1. Pregnancy Issue (D) 2. Sedation, dizziness 3. Can induce Hepatitis/hepatic fail, pancreatitis, abnormal bleeding 1. Pregnancy Issue (D) - spina bifida 2. GI, dizziness, Agranulocytosis 4. Hepatitis/cholestatic jaundice 5. Steven Johnson
Antitussives and Mucokinetic Agents (Coughing) Codeine Hydrocodone Dextromethorphan Centrally acting 1. Non-specifically reduce excitability of cough antitussives center (anodynes) 1. Non-productive cough 1. Resp depression - caution in < 2 - when cough results in sleep loss 2. Constipation, miosis, sedate, addict - to prevent herniation, spread of infection Fewer side effects - Confusion, excitation, nervous, resp depression in high dose - high abusive potential
Reduce afferent inputs to the cough center - on stretch receptors in the respiratory passage Stimulate/modify mucous production in bronchi stomach irritant that causes bronchial secretion Break down sputum aggregates to smaller parts splits disulfide bonds - Nebulize 1. Productive coughs - Expectorants - thick/tenacious cough secretions - Mucolytics - cystic fibrosis, antidote to acetaminophen poisoning
1. Can cause hypersensitivity rxn procain/tetracaine 2. DON'T CHEW - anesthesia GI tract issues
secretions - Mucolytics - cystic fibrosis, antidote to Clinical Use/Indications acetaminophen poisoning ADHD Meds
Adverse Effects
Common Name
Sub Category
Mechanism of Action
Adverse Effects
Chlorpromazine Prochlorperzine Promethazine Thiethylperazine Droperidol Scopolamine Diphenhydramine Dimenhydrinate Hydroxyzine Meclizine Promethazine (phenergan) Ondansetron Granisetron Dolasetron Polonosetron Trimethobenzamide Metoclopramide
Antipsych
1. Depresses excitability of the CTZ by blocking D2 receptors and transmission 2. Also peripherally blocks D2 in GI
1. Radiation/drug induced vomiting 2. Thiethylperazine used for post-op 3. Doperidol has tranquilizing effects
Anticholinergic Blocks Ach receptors in CTZ, vest nuclei and GI tract Antihistamines - Blocks Ach receptors in vest nuclei and CTZ Ethanolamine Antihistamine1st gen pipera Antihistamine phenothiazine Serotonin Selectively blocks serotonin receptors (5-HT3) in blockers GI and CTZ
Sedation, blurred vision, reduced GI/bladder tone Sedation, blurred vision, dry mouth 1. Pregnancy issue 1. Contraindicate in children
1. Post-op n/v following highly emetogenic surgery 2. drug-induced n/v (antineoplastics) 3. Radiation therapy n/v 4. NO motion sickness 1. Post-op n/v and coughing 1. GE reflux 2. Daibetic gastric stasis 3. N/v assoc w/ cisplatin, radiation N/v due to antineoplastics Anorexia w/ weight loss in AIDS
Benzamide derivatives
Antiemetic - depresses CTZ (D2) Antitussive - suppresses laryngeal reflex 1. Prokinetic 2. Anti-emetic - antagonism of dopamine Vestibular Potent CYP3A4 inhibitor
1. CNS depression 2. EPS, Reye's syndrome 1. CNS depression 2. EPS Impairs cognitive and motor fx
Dronabinol Aprepitant Aplprazolam Triazolam* Lorazepam* Oxazepam Flurazepam Prazepam Diazepam* Pehnobarbital Mephobarbital Pentobarbital Secobarbital
Sedative-Hypnotic Drugs Benzodiazepein 1. Binds to site on GABA A receptor, which es (short acting) enhances GABA's effect 2. Mediates both sedation and memory effects 3. Benzo + GABA = increased freq of channelopening events (Cl-) Benzodiazepein es (long acting) 1. Anxiety 2. Spasticity 3. Status epilepticus (lorazepam, diazepam) 4. Detox 5. Night terrors, sleepwalking 6. Insomnia (estazolam, fluraz, quaz, tema, triazolem) - bind 3 alpha-1 sybtype 1. Anticonvulsant - seizures 2. Basal anesthesia 3. Narco-analysis 4. Decreases respiration neurogenic/chemical/hypoxic drives 1. Potential abuse - lethal:effective dose = 200:1 2. Withdrawal 3. Daytime drowsiness 4. Respiratory impairment
Barbiturate Sedativehypnotics
1. Barbiturates + GABA = increased duration of channel-opening events (Cl-) -> decreased neuron firing
hypnotics Common Name Thiopental Chloral hydrate Diphenhydramine (Benadryl) Trazodone Ramelteon Zolpidem (Ambien) Zaleplon (Sonata) Eszopiclone (Lunesta) Historical Antihistamines Antidepressan Sub Category
Melatonin agonist Imidazopyridine Act on alpha subunit of GABA A - selectively bind Insomnia derivative to receptor to produce hypnotic effects Pyrazolopyrimid ine class Antidepressants
Fluoxetine (Prozac) Sertraline (Zoloft) Paroxetine (Paxil) Citalopram (Celexa) Escitalopram (Lexapro) Fluvoxamine Imipramine Desipramine Amitripltyline Nortriptyline Venlafaxine (Effexor)
1. Selectively block uptake of serotonin 2. Advantages - more benign than TCAs, no quinidine action on heart, no significant weight gain 3. High safety margin
1. Transient - nervousness, insomnia, nausea, diarrhea 2. Persistent - sexual dysfx 3. Serotonin syndrome - confusion, fever, altered consciousness, myoclonus 4. Inhibits p450
Tricyclic 1. Block active reuptake of norep and serotonin antidepressants higher levels in synaptic cleft (TCA) 2. Original gold standard
1. Resistant depression 2. Enuresis in childhood (Imipramine) 3. Chronic pain, neuralgias, miagraine, diabetic neuropathy 1. Depression, GAD, Panic 2. PTSD, PMS
1. Sedation, anticholinergic 2. ECG change 3. Weight gain, impotence 4. Can precipitate mania Similar to SSRIs
Duloxetine
Serotonin + Reuptake inhibitor of serotonin, norep, and some Norep reuptake dopamine inhibitors (SNRI)
Phenelzine
MAO inhibitors Inhibits MAO A and B non-selectively, which result in higher norep and serotonin release
Tranylcypromine Buproprion (Wellbutrin, Zyban) Norep + Blocks reuptake of norep and dop dopamine reuptake inhib (NDRI) Noradrenaline + serotonin (NaSSA) Serotonin antag reuptake inhibitors (SARI)
1. Better for bipolar/atypical depression 2. Phobias 3. Migraines 4. Neurodermatitis 1. Depression (fewer sex side effects) 2. Smoking cessation - Zyban 3. ADHD
1. Weight gain, sexual dysfx 2. Hepatotoxic 3. Slower onset Sexual dysfunction Faster onset 1. Agitation, insomnia, seizures 2. Inhibits 2D6
Mirtazapine Nefazodone
Adverse Effects
Common Name
Sub Category
Mechanism of Action
Adverse Effects
Nitrous Oxide (N2O) Halothane Enflurane Isoflurane Desflurane Sevoflurane Ketamine Propofol Etomidate
Gases
CNS depressants - blood soluble = rapid induction/recovery - lipid soluble = potency = 1/MAC - ventilation + concentration = more rapid uptake
Must combine w. IV narcotics, barbiturate 1. Bone marrow suppression in high conc and relaxants 2. Neuropathy 1. Massive hepatic necrosis (halothane hepatitis) in 1/35,000, less in children 2. slows HR, decreases MAP/CO 1. Free F- released = renal fail (preexist) 2. Increases HR, decreases MAP/CO 1. No renal dysfx, minimal metab 2. Increases HR, decreases MAP/CO + SVR 1. Minimal liver biotransform 2. Increases HR, decreases MAP 1. Same as enflurane - disolve in soda lime 2. Little heart effect
IV agents
Local Anesthetics Bupivacaine Ropivacaine Lidocaine Tetracaine Cocaine Procaine Benzocaine Intraocular Pressure (IOP) Lowering Agents - Ocular Hypertensives Brimonidine Timolol Dorzolamide hydrochloride Acetazolamide Mannitol Glycerin Isosorbide Pilocarpine Echothiophate iodide Latanoprost Prostaglandins Miotics Direct - stimulate muscarinic receptors to cause constriction and increase flow Indirect - blocks Ach-esterase F2 - increase matrix turnover = increased flow Alpha agonists Beta blockers Carbonic Anhydrase Inhibitors Hyperosmolar agents Activates alpha 2 - inhibits aqueous secretion Blocks beta receptors - decrease aqueous secre Inhibits CA, which decreases aqueous production 1. Open angle glaucoma 2. Ocular hypertension dry mouth, hypotension, lethargy Bradycardia, bronchospasms, fatigue, worse myasthenia gravis Drops - bitter taste, diuresis, fatigue, StevensJohnson Oral/IV - hypokalemia, renal stones, aplastic anemia, Stevens-Johnson CHF, urinary retention, back acne, MI vomiting, less CHF, similar to mannitol same as glycerin, but safer in DM Angle closure, breakdown of barrier, retinal tears - don't use in young patients Retinal detachment, myopia, angle closure Increase melanin, blurred vision, URI symptoms, myalgia Esters Amides 1. Blocks voltage dependent Na channels - block AP 2. Absorption - short = limited, need vasoconstrictor 3. Vasodilate except for cocaine 4. Esters metab by pseudocholinesterases, Amides by hepatic microsomal enzymes 1. Minor surgery 2. Spinal anesthesia 3. Regional anesthesia 4. Infiltration anesthesia 5. Post-op analgesia 1. CNS - lightheaded, restless, tonic-clonic 2. CV - cocaine = htn, mi, cerebral hemorrhage 3. Allergy - esters 4. Treat convulsions w/ diazepam or barbiturates
Sub Category
Mechanism of Action
Adverse Effects Cystoid macular edema, mydriasis, blurred vision, tachycardia, htn, headache
Common Name
Sub Category
Mechanism of Action
Adverse Effects
Penicillin, etc Non-steroidals/ Corticosteroids Tropicamide Atropine sulfate Phenylephrine Macugen Lucentis Avastin Acetaminophen Aspirin Naproxen Isometheptene (Midrin) Metoclopramide Sumatriptan Zolmitriptan Naratriptan Rizatriptan Almotriptan Frovatriptan Eletriptan Ergaotamine Dihydroergatamine Chlorpromazine Propranolol Timolol Divalproex Topiramate Verapamil Flunarizine TCAs
Antibacterials
Self-explanatory
Antiinflammator y Dilating drops Parasympatholytic - block Ach receptors in iris ciliary body - mydriasis and cycloplegia Sympathomimetic - stimular dilator muscle Anti-VEGF
Eye drops
Pegylated oligonucleotide binds to VEGF 165 and Stops angiogenesis/neovascular in: prevents ability to bind to receptor 1. macular degen (wet), DM retino 2. Neovascular glaucoma, retinal vein Recombinant fragment that ragets VEGF-A occlusion Parent of Lucentis Migraine Drugs Mild-moderate migraines Just helps with the pain
1. Blurred vision, pain, redness of eye, increased IOP, retinal detachment 2. Dizziness, headache, nausea, diarrhea 3. Beware hypersensitivity rxn
Analgesic NSAIDs
Combine to prevent migraine Good for nausea and vomiting Triptans 1. 5-HT1B/D agonists, some 1F (1B = bv, 1D/F = neurons) 2. Selectively constrict cranial vessels and reduce inflammation 3. Block pain transmission from CN V to trigeminal nucleus caudalis 4. All except sumatriptan are more centrally penetrant Abort Moderate-Severe migraines If doesn't abort in 2-4 then medication won't help 1. Contraindications - Heart disease/MI - Angina, HTN - basilar migraine 2. Triptans can't be used w/ other triptans or ergot or MAOIs 3. Too much ergot = poisoning
Ergot alkaloids 1. 5-HT1B/D agonists 2. Additional receptor affinities Neuroleptics Opioids Beta blockers Anti-epileptic Ca blockers Antidepressants Without sympathomimetic activity GABA agonists Prolonged migraine + signif n/v Don't respond to normal tx Migraine prevention Safe for pregnant when limited 1. Decreased sexual activity, bradycardia, lethargy Pregnancy group D, liver issues Significant cardiac (Class 4 antiarrhy) Severe cardiac effects, orthostatic hypotension
Common Name
Sub Category
Mechanism of Action
Adverse Effects
Levodopa
Levodopa
Trihexyphenidyl Benztropine Bromocriptine Pergolide Pramipexole Ropinirole Apomorphine Entacapone Tolcapone Selegiline Rasagiline Amantadine Antipsychotics Reserpine Tetrabenazine Botulinum toxin
Dopamine replacement - absorbed in SB through LNAA - converted to dopamine + O-methyl dopa by DDC Anticholinergic Blocks central muscarinic receptors Dopamine agonist Stimulate dopamine receptor directly
Nausea, hypotension, hallucinations - Must be administered w/ carbidopa, a DDC inhibitor Mild tx for Parkinson's - tremor + rigidity dry mouth, sedation, blurry vision, urinary retention Moderate tx for Parkinson's - tremor, rigidity, bradykinesia PUD, vasoconstrictive, pulm fibrosis, hallucination, valve disease (pergolide) Somnolence, leg edema, compulsive behavior
COMT inhibitors MAO-B Inhibitors Other Dopamine Receptor Blockers and Depleters Poison
Inhibit breakdown of dopamine by COMT Inhibit breakdown of dopamine by MAO Dopaminergic, anticholinergic, NMDA antag
Adjunct w/ L-dopa - increases ON time Mild tx - tremor, rigid, bradykinesia, potentially neuroprotective Mild tx - tremor, rigid, bradykinesia
Orange discoloration of urine, diarrhea Fatal hepatitis Serotonin syndrome w/ SSRIs Peripheral edema, hallucinations
Focal dystonia - cervical dystonia, blepharospasm, hemifacial spasm Antiepileptic drugs Tx of choice for acute seizures Refractory status epilepticus Partial seizures
Lasts 3-6 months - could overweaken muscles Sedation, resp depression bad side effects- only use in infant, poor Can cause absence epilepticus, sedation Thrombophlebitis, sedation, dizziness, diplopia, hepatotoxicity, myelosuppression
Benzodiazepines Barbiturates Tiagabine Phenytoin Carbamazepine Oxcarbazepine Lamotrigine Lacosamide Ethosuximide Valproate Topiramate Zonisamide Levetiracetam Gabapentin/Pregabalin
GABA affecting GABA-A - Cl channel opens more GABA-A - Cl channel opens longer Selective GABA reuptake inhibitor Na channel effecting
Enhances the slow inactivated state of channel Enhances slow inactivation of the channel Ca channel Blocks T-type Ca channels in thalamus - stops affecting abnormal thalamic excitability Multiple MOAs 1. synaptic GABA, 2. NMDA excite 1. Cl events, 2. glutamate, Ca channels 1. Na channels, 2. Ca channels, 3. CA inhib Unique MOAs Binds vesicle protein SV2A - unknown a2 subunit of Ca channels
Good for all seizures Only absence seizures Good for all seizures All except absence seizures Good for all seizures Good for all seizures Partial seizures - pain
Headache, insomnia, rash Sedation, dizziness, headache, behavioral, myelosuppression Cog impairment, weight gain, hair loss, tremor, bad for pregnant Very safe - paresthesias, cog impair, weight loss Typical side effects, decreased appetite Safe - sedation, irritability Mild - sedation, weight gain
Common Name
Sub Category
Mechanism of Action
Adverse Effects
Alcohol
Binds GABA, dilates bvs, decreases glutamate, reduces ADH secretion CNS/resp depression, miosis 1. CNS/resp depression, lethargy, coma 2. GHB - agitation, seizure, brady, amnesia 3. Chloral - dysrthmias 4. Withdrawal - insomnia, n/v, sweat, tachy 1. HR/BP, euphoria, strokes, rhabdomyolysis, seizures, renal fail Euphoria, hallucin, tense jaw, bruxism Euphoria, panic attacks, paranoia Tachy, htn, ataxia, seizure, coma drowsiness, euphora, paranoia Euphoria, dysrythmias, met acid transient euphoria, CNS depress Treats diarrhea/intestinal colic Neonatal opioid dependency Analgesic, dyspnea due to PE Mild/moderate pain, antitussive Schedule 1, 3x more than morphine Parkinsons oral analgesic moderate/severe pain
Heroin/Morphine Barbiturates Benzodiazepines Chloral hydrate GHB Cocaine Ecstasy LSD Phencyclidine (PCP) Marijuana Hydrocarbons Nitrous Oxide (N2O) Paregoric Morphine Codeine Heroin Apomorphine Oxycodone Hydromorphone Meperidine Fentanyl Diphenoxylate Loperamide Methadone Darvocet Pentazocine Nalbuphine Naloxone Naltrexone Buprenorphine
Opioids Sedativehypnotics
Binds to mu receptors 1. Enhance GABA 2. GHB - odorless, colorless 3. Chloral hydrate - pear-like odor
Wenicke, Korsakoff, cirrhosis, PUD, fetal alcohol syndrome, pancreatitis - BAD w/ acetaminophen Tx: ABCs, Narcan for acute, supportive Treatment: 1. Supportive care 2. Phenobarb - urine alkalinization 3. Chloral - beta blokcers 4. Benz - Flumazenil Treatment: supportive Hyperthermia - ice, Seizures - Benzo, phenobarb HTN - sodium nitroprusside, phentolamine Treatment - supportive
Stimulants
1. Block presynaptic reuptake of dopa, norep, serotonin 2. Produces vasoconstrict and local anesthetic Interacts with serotonin receptors Related to ketamine - CNS depressant
Hallucinogens
Inhalants
CNS depressants
Chronic: met acidosis, hypokal Chronic: polyneuro, mega anemia 1. Seizures (Meperidine) 2. Depress resp 3. Emetic effect - n/v 4. Miosis (morphine) 5. Antitussive - lower dose than analgesic 6. Bowel dysfx/constipation 7. CV - hypotension/brady 8. Euphoria, sedation 9. Dependence
Naturally 1. Inhibit firing of neurons in dorsal horn, limbic occuring opioid structures and cerebral cortex agonist 2. adenylyl cyclase -> cAMP -> Ca influx or K efflux -> neurotransmitter release 3. Targets mu receptors Semi-synthetic agonist
Synthetic agonists
Not antitussive, local anesthetic Post-op/chronic pain, anesthesia Diarrhea acute, non-specific diarrhea mod/severe pain, opioid dependency No clinical usefulness
Potential abuse, psychotomimetic, hallucinatory and dysphoric effects Need to assist resp depression w/ vent Liver toxicity Reduction in bowel dysfunction, constipation
Pure antagonists Binds all opioid receptors with higher affinity than Antagonize opioid effects agonist and reverse effects of agonists Treat opioid dep, alcohol, detox Partial agonist Mu Agonist to a ceiling, submaximal response PAMOR antagonists Analgesic effect
Other
Other
Drug interact: - DAMN (Dehydrate, AceI, Metro, NSAID) - COAST (CA inhib, Osmotic, Antacid, Salt, Caffeine)
Drug interact - aspirin, felbamate - Rifampin Induces own metabolism watch hepatic enzyme Be careful of asians
Opioids - doses < for cough vs analgesia Non-opioid - d-isomer of codeine - don't use with MAOIs
Other
Other
Pentothiazine derivatives
1. Antacids decrease absorp 2. Antihist/barbit/ETOH increase depression 3. CYP450 except loraz, oxaze, temaz
Other
25-50 mg hs
Takes a long time to reach steady state Shorter half life, better More sedating, better for anxiety
If overdosed (cardiac monitoring) use gastric lavage, NaHCO3, Lidocaine or Phenytoin 1. Liver metabolized 2. Dose dependent HTN Less risk of liver issue, can treat Diabetic neuropathy 1. Tyramine food, amphetamines -> HTN crisis
Other
Other
Nonvolatile 1. Depressed heart contractility 2. Decreased smooth muscle tone, PVR, TV 3. Blocks vent response to hypoxia
More rapid recovery than barbiturates Minimal CV effects Long acting Medium Acting Long duration Medium + surface Short duration Surface Don't use in kids Don't use w/ sulfa allergy, hyponatremia/kalemia, thiazides or digitalis
ure
ymptoms, myalgia
Other
Other
Oral, subQ, nasal liver/renal Oral, nasal - liver Oral - renal Oral- no renal/liver Oral - liver Oral - renal Oral - liver Oral - only 2x/wk IV/nasal - avoid preg
Not in US
Other
Lorazepam/Diazepam Phenobarbitol (IV) Nonlinear pharmaco SJ syndrome, asians Not as bad Good for Preg women New drug
Hepatic failure, polycystic ovary ight loss Works fast Short half-life
Other
henobarb mine
Schedule IV drugs