Stuff Highlighted in the review

Barbiturates Bind to ​GABA​A​ ​receptor and ​Inc the duration ​(“​Barbi​durat​es=Inc ​Durat​ion”)​ of Action of GABA.
Independent of GABA​. marked ​CNS depressant​. ​Has a very​ LOW margin of Safety.
Pento​barbital Has ​Abuse​ potential.
(Nembutal Sodium®) Have been replaced therapeutically by benzodiazepines.
Phenobarbital​ (Luminal CNS depressant effects​ w other depressants are ​supra additive esp w ​Alcohol
Sodium®) Barbiturates (​acids​) can be ​cleared w alkalinization​ of the urine​.
Secobarbital (Seconal®) Pk-​ oral, enter CNS quickly, Metabolized in Liver, ​CYP450
Uses-​ ​anticonvulsants​, Dec GI spasms, in general use is rare.
SideFx- ​CNS depression, Paradoxical excitement, ​Respiratory Depression​, INC ​porphyrin
synthesis, ​Withdrawal can be life threatening​.
CI​- any form of ​porphyria!!!​(abnormal heme synthesis), P ​ ulmonary insufficiencies​.

Benzodiazepines Most common group of ​anxiolytics​ and sedative-hypnotics. Produce CNS depression
Some are anticonvulsants (clonazepam, lorazepam, diazepam).
Diaze​pam​ (Valium®) “Fre​nzodiazepines= Inc ​Fre​quency”
MoA-​ bind a sp receptor assoc w GABA​A​ receptor complex. ​Intensify the actions of GABA-​.
Chlordiazepoxide
Only ​act in the presence of GABA. ​Ceiling​ effect​. Less respiratory depression thus ​Relatively
(Librium® )
Safe Drugs.
Alprazolam​ (Xanax®)
Pk-​ converted to ​active metabolites​ which are metabolized very​ slowly. D ​ uration of Action is
Lorazepam (Ativan®,
proportional to elim of metabolite not the drug itself. May ​persist in body​ for long time thus
Alpazam®)
provides a ​Tapering​ response helpful in Alcohol withdrawal. ​Elderly​ do NOT metabolize benzos
Oxazepam (Serax®)
well and should get a lower dose.
Clonazepam (Klonipin®)
Long​ ​acting metabolite. ​Short ​acting and used in brief surgical procedures.
Midazolam​ (Versed®)
(“ATOM-Alprazolam, Triazolam, ​Oxazepam​, Midazolam”)
Flurazepam​ (Dalmane®) DIs-​ ​Extensive Liver Metabolism​, Do NOT induce liver enzymes thus have ​fewer drug
Estazolam (Prosom®) interactions. Cimetidine→ inc T1/2 of diazepam.
Temazepam​ (Restoril®) Uses-​ ​Anxiety​ (Except in OCD,Agoraphobia, PTSD, and kids- should use antidepressants
Triazolam​ (Halcion®) instead). ​Insomnia​ (“​Z drugs” are better ​tho) ​hangover​, ​middle​, ​short-​ just help get to sleep.
Epilepsy/seizures- (​Diazepam​ IV ​for​ status epilepticus​). Sedation/Amnesia/Anesthesia
(​brief surgical​ ​procedures). ​Muscle relaxation​. Acute ​Withdrawal​ from alcohol and
Barbiturates.
SideFx- ​Excess ​sedation​ and ​memory loss (​esp in elderly​).​ CNS depression exacerbated w
Alcohol. Can have some ​dependence​ if used chronically. If used chronically- seizure can occur
during withdrawal.
CI-​ ​Prego, Kids, Sleep apnea.
OD-​ Fatalities may occur ​if combined w Alcohol​.

Benzodiazepine Competes for Benzo receptor.

Pk-​ Given slowly over 3min IV to minimize ​seizure risk.
antagonist
Use-​ to ​reverse effects of benzos​ (midazolam) following surgery. Also reverses effects of other
drugs that act on Benzo receptors (Z drugs).
Flumazenil
Sidefx-​ ​Withdrawal and ​seizures
(Romazicon®)
CI- ​if there are any signs of seizure disorders.

Z​olpidem​ (Ambien®; Bind to ​B​Z​1​ subtype of benzo (GABA) receptor. Very strong/​rapid​ ​Sedation​. Preserve deep
Intermezzo®; Zolpimist® sleep w only minor effect on REM.
(spray);Edluar®(subling Long term ​tx of insomnia​. ​The other 2 are for short term insomnia but often used chronically.
ual)) Pk-​ CYP3A4, ​short half life​ metabolized by ​aldehyde dehydrogenase- cimetidine​ will inhibit
Z​aleplon (Sonata®) as well as CYP3A4. ​Use Half Dose for Women. ​May have some drowsiness due to ​longer​ half
Es​Z​opiclone​ (Lunesta®) life.
Sidefx- GI probs, ​Sleep Related behaviors​ ​(night wandering ect.8..), Rebound Insomnia,

Ra​melt​eon​ (Rozerem) Melatonin MT1 and MT2 ​receptors- ​regulate sleepiness​/ circadian rhythms.
Tasi​melt​eon​ (Hetlioz®) Shorten delay to sleep onset. No effect on REM
DI- CYP inhibitors
“Melt to sleep” Sidefx- few,​ may inc liver enzymes
CI- severe liver dz.

Suv​orex​ant (​Belsomra​) Antagonist at ​Orex​in​ Receptors (​orexins regulate sleep wake cycle/ promote wakefulness).
CI-​ ​Narcolepsy

Diphenhydramine Antihistamines. ​Used in ​OTC​ preparations as sleep aids (ie Tylenol PM) . Useful for occasional
(​Benadryl®​) insomnia.

Anxiety drugs

Buspirone (BuSpar®) First drug class to​ relieve anxiety w/o producing sedation.​ Acts as a​ Partial agonist at
5-HT1a. ​“If you get anxious ​on​ the ​Bus ​take ​Bus​pir​on​e to feel better”
Full effect takes ~2wks ​to develop. ​Low addiction Potential.
Will NOT prevent symptoms of Benzo/ alcohol withdrawal (​bc it doesn’t act at GABA)
DI- CYP3A4, May get​ inc BP in pt using ​MAOIs​, use cautiously w drugs that inc serotonin.

Kava Used for mild anxiety. Can cause ​Severe liver toxicity​. Do NOT use in pregnancy

Valerian Mild anxiolytic. ​Hepatotoxic​. CI in Prego.

B-Blockers Used for ​Performance anxiety.

Ethanol Dec risk of Heart attack. Abuse potential→ ​Alcoholics​.

MoA-​ ​CNS depressant​ by interacting w ​GABA​ receptor to inc Cl influx. ​Long Term use→
down reg GABA receptors.
Inhibits​ effect of excitatory aa ​glutamate on ​NMDA​ receptor​. ​stimulant​ (inhibits inhibitory
path) → disinhibition. Chronic use→ ​Upregulation of NMDA receptors​.
CNS depressant and ​Sedative​. Impairment of ​intellectual and motor function​. Some
amnesia​.
Dose response curve is ​Steep​ (only 5x diff can be fatal).
Pk- absorbed in stomach and SI. Faster on empty stomach. Metabolized by ​alcohol
dehydrogenase (M​>F) . Crosses ​BBB​ and p ​ lacenta​.
Metabolism- ​10g/hr​ (zero order kinetics). Chronic use induces ​CYP2E1 (​ ​inc conversion of
acetaminophen​ to a t​ oxic​ metabolite)​.
Probs-​ Liver damage. Ketoacidosis, Hyperlipidemia, Fatty liver, Lactic acidosis→ gout.
Effects- ​disinhibition, dec anxiety, mild euphoria, sedation, impaired speech, ataxia.
Pharmacodynamic tolerance is due to down reg of GABA receptors and maybe upreg of NMDA
 receptors. Smooth muscle-​Vasodilator​→ ​hypothermia ​(Cutaneous flushing). Kidneys-
diuretic​.
Toxicity-​ 200-500 mg, Emesis-stupor-coma-respit depression-possible ​death​.
If seizures occur tx w ​Phenytoin​.
Chronic Use​- ​malnutrition​ (lots of empty calories, ​Folate and Thiamine def​., ​Gastritis,
Pancreatitis, Hepatotoxicity​ (Fatty liver→ fibrosis. Alcoholic hepatitis. Liver damage faster in
women), CV-(​Binges→ arrhythmias​, Cardiomyopathy, HTN), ​Fetal alcohol synd​.
Testicular atrophy, Korsakoff psychosis, wernicke encephalopathy ​(Exacerbated by
thiamine def.)
Tolerance/Dependance-​ both to the ​effects​ (​pharmacodynamic​) and Due to Inc ​metabolism
(​pharmacokinetic​). ​Severe withdrawal synd. Lethal dose is NOT changed.
Alcoholism- ​drink despite adverse consequences. Some ​Genetic​ assoc. ​B-endorphins​ in the
dopamine reward path​.
Withdrawal​- goal is to ​prevent seizures​, DTs and arrhythmias. Use ​long acting ​benzos​ to ​taper
the withdrawal.
Chronic tx of alcoholism-​ after withdrawal, combo of drugs and psychosocial txs. Long term

Naltrexone ​(ReVia®; Opioid receptor antagonist​. Stim dopaminergic reward path. Blocks the ability of alcohol to
Vivitrol®) stim this reward path→ ​reduces cravings​ for alcohol. Dec rate of relapse by 50%.
Sidefx- ​nausea, ​Liver damage​, other opioids not effective,
Nalmefene (Revex)- longer action, ​less ​likely to cause ​liver damage

Acamprosate ​(campral Structural analogue of GABA.​ helps ​restore the normal balance of GABA​ and glutamate
EC) transmission. Decreases EtOH intake. Decreases likelihood of relapse.
NO liver toxicity​.

Topiramate (​topamax​) Anticonvulsant. Decrease craving for alc

Disulfiram (Antabuse) Blocks aldehyde dehydrogenase. If taken w alcohol→severe sickness/vomiting.

Has a long duration (cant drink for 4-5days).
DI- metronidazole, come cephalosporins, and oral hypoglycemic agents.
Dangerous​ and NOT recommended.

Gabapentin An anticonvulsant

Ondansetron An antiemetic.

Non pharm tx of AA excellent social help.

alcoholism

Methanol Is converted to alcohol dehydrogenase to ​formaldehyde​ (toxic) ​and then to formate.

Ss of toxicity→ visual disturbances.
Tx - ​Fomepizole ​(alcohol dehydrogenase inhibitor​) & ethanol will compete w alcohol
dehydrogenase to dec form of formaldehyde.

Ethylene glycol Metabolized by ​alcohol dehydrogenase

(antifreeze) toxicity→ metabolic acidosis.
Tx - ​Fomepizole ​(alcohol dehydrogenase inhibitor)
Seizures Abnormal discharges of electrical activity of ​cerebral cortex​. Epilepsy=recurrent.
Partial seizures- ​simple​(short, conscious), ​complex ​(longer, impaired consciousness)
Generalized seizures- ​Tonic clonic​ (grand mal, LoC, jerking), ​Absence ​(petit mal,
staring,<30sec, altered consc.) ​Myoclonic ​(brief-like a muscle shock)
Mech- ​underactivity of GABAergic neurons, or overactivity of glutamate transmission
Also assoc w Na and Ca channel activity.

​ artial seizures​ ​and g

Drugs used in​ p ​ eneralized tonic-clonic seizures
-act on Na channels

Phenytoin ​(Dilantin®) Block High freq repetitive firing​ by prolonging inactivation of Na channel.
Fosphenytoin Tx for​ Partial seizures and generalized tonic-clonic seizures.
(Cerebyx®) NOT Absence.
Pk- ​Oral ​(not water sol).​ Is used as ​Injection​.​ ​Elim is dose dependent ​(1st order) at low blood
levels, but zero order at therapeutic range​.
DI-​Warfarin, Induces microsomal enzymes, ​Carbamazepine​→​ inc metabolism of phenytoin.
Sidefx-​Gingival Hyperplasia​ & Hirsutism, ​PregoD​, ​Risk Steven Johnson Synd​ (​SJS​).

Carbamazepine Inhibits Na channels and dec transmitter release.

(Tegretol®) DOC for Partial seizures. ​Also used for ​generalized tonic-clonic. ​Also used for bipolar and
trigeminal neuralgia.
Pk- Induces hepatic enz (CP3A4)
DI- inc metabolism of ​Phenytoin, Ethosuximide and valproic acid
Sfx- ​PregoD, SJS (assoc w HLA-B 1502), diplopia, Ataxia, blood dyscrasias​.

Phenobarbital Prolongs opening of GABA​, used for ​Partial and generalized tonic clonic seizures.
(Luminal®) Sfx- ​PregoD

Lamotrigine Inactivates voltage dependent Na channels→↓glutamate activity.

(Lamictal®) For ​Partial seizures (adjunct tx).
For absence in kids.
Sfx- CYP450, ​PregoC, SJS, ​diplopia

Gabapentin GABA analog.

(Neurontin®) Used as​ Adjunct tx ​for​ partial and generalized tonic-clonic seizures.
Also for​ Neuropathic pain.
Sfx- ​PregoC

Topiramate Inhibits voltage dependent Na channels. Enhances GABA​A​ currents.

(Topamax®) Inhibits spread of seizures. And for ​prevention of migraines
Use-​ ​Broad spectrum​- Pt/T-C/absence​ ​seizures​.
Sfx- ​Myopia/ Glaucoma​/ ​Wt loss​.

Levetiracetam Binds ​SV2A protein of both GABA and glutamate neuron

(Keppra®) Use- ​Partial​, myoclonic, general T-C seizures.
Minimal Drug interactions​(NO CYP 450)=good for ​Adjunct t​ x.

Tiagabine (Gabatril®) Inhibits GABA (GAT-1)​.

 Good adjunct tx​. (minimal drug interactions.)
Sfx- rash is rare, PregoC

Vigabatrin (Sabril®) Last resort! Inhibits GABA-T.

For adult​ complex partial seizures ​and ​Infantile spasm.

​ ork on Ca channels
Drugs for​ ​Absence Seizures. W

Etho​sux​imide(​Zarontin​) DOC for ​Absence​ seizures​. ​Reduces low threshold Ca currents​.

Clearance is dec by Valproic acid.
Sfx- ​Hiccup​, ​SJS-rare​, ​PregoC.
“It ​sucks​ to have ​s​ilent ​s​eizures”
“EFGHIJ ​E​thosuximide→ ​F​atigue, ​G​I distress, ​H​iccups​, ​I​tching, s​J​s”

Valproic acid Blocks high-freq repetitive firing​- (​inhibits Na channels)​. ​Inc ​synthesis and levels of ​GABA
(Depakene®) Use- ​mixed seizures​ (absence, generalized T-C)- ​DOC if both are occurring together​.
Also for Bipolar and migraine prophylaxis
Sfx- ​weight gain, Hepatotoxicity,​ SJS, PregoD
DI- inhibits its own metabolism/ phenytoin/ carbamazepine.

Clonazepam A Benzo. For ​Absence seizures​.

(Klonopin®) Sfx- ​sedation common, PregoD

Stevens-Johnson Toxic epidermal necrolysis​ (autoimmune rxn). Assoc w ​HLA-B ​1502. ​Hypersensitivity rxn​-
Synd can be fatal.

Drugs used for​ ​Status Epilepticus

Diazepam(Valium) DOC ​for​ Status epilepticus​.

Lorazepam (Ativan) Given IV.

Anticonvulsants and Most cause​ birth defects. ​Many ​dec effectiveness of Birth control.
Pregnancy For women w epilepsy​- 2x risk (even w/o drug tx) for kids w birth defects.
Congenital heart defects, Neural tube defects.
Tx- give supplemental​ folate and Vit K.

Tricyclic MoA- ​Inhibit Uptake of NE and 5HT​, also block M/α/H receptors. NO euphoria-just ​normal​,
take ​2-3 to be effective​. Can be used in prego.
Antidepressants
Ami/Imi→ more sedating. Nor/Des→ less sedating.
(TCAs) Sfx- CNS (drowsy, ​sedation​, impaired memory, A ​ nalgesia m/c​ ​use ​now.) C​ ardiac (​Torsade
Tertiary Amines de pointes​, α block​-postural hypotension, tachycardia​, ​Least cardiotoxic​.​) Cholinergic effects,
Imipr​amine​ (Tofranil®) weight Gain​. ​dec ​seizure t​ hreshold​. S
​ IADH-​hyponatremia​, ​Sexual dysfunction​, tolerance,
Amitriptyline​ (Elavil®) Uses- depression, panic,​ chronic P ​ ain​, F​ ibromyalgia​, ​Enuresis ​(bedwetting)-imipramine,
Trimipramine(Surmontil) ADHD,​ OCD
Doxepine (Sinequan®) Tx of OD- ​Phenytoin ​for arrhythmias.
Clomipramine DI-​ ​MAOIs→ ​serotonin synd​., ​Fluoxetine ​(SSRIs)→toxicity.
(Anafranil)
​Secondary amines
Desipramine​(Norpramin “Tri-Cs=Cardiac, Convulsions, Coma”
)
Nor​trip​tyline ​(Pamelor)
Protriptyline (Vivactil®)

Monoamine Last resort!!!

Pk- oral. ​Irreversible ​inhibition of MAO.
Oxidase
Sfx- accum of ​Tyramine→ ​HTN crisis​ (​Tyramine​ in foods (​alcohol, sauerkraut, sausage, aged
Inhibitors(MAOIs) cheese)​ )
Phenelzine (Nardil®) Other sfx-​ weight gain, Anticholinergic effects​.
Tranylcypromine DI- ​Sympathomimetics/ Buspirone→​severe HTN​, TACs/SSRIs→​serotonin synd​.​,
(Parnate®) Meperidine, Tramadol, Dextromethorphan (​opioids​)​→serotonin synd.

Selective 1st-​DOC for Depression, . ​Inhibit reuptake of 5 ​ HT​. Effect takes ~2-3 wks. Mild sfx.
Pk- Long-lasting. ​Fluoxetine/Paroxetine inhibit C ​ YP2D6.​ D​ ec activity of some opioids. Dec
Serotonin
activation of ​Tamoxifen ​(breast cancer tx).
Reuptake Use- ​Depression​, Panic disorder, OCD, Social anxiety, Bulimia, alcoholism.
Inhibitors (SSRIs) Sfx- ​GI​-nausea​, Wt loss initially→ wt gain, CNS stim, ​Sexual dysfunction​, SIADH - poss
Fluoxetine​ ​(​Prozac®​) hyponatremia, Photosensitivity.
Fluvoxamine (Luvox®) DI- ​MAOIs​, St John's wort, amphetamines, TCAs, Warfarin, Phenytoin/Carbamazepine,
Paroxetine ​(Paxil®) ßblockers, ​Opioids Less effective​, Tramadol→seizures, ​Tamoxifen.
Sertraline ​(Zoloft®) Long​ duration of effect​, wait ​5wks(to get rid of)​ post before switching to MAOI, may cause
Citalopram ​(Celexa®) Insomnia​, taken ​Weekly​.
Escitalopram Similar effects, OCD/social anxiety, shorter duration of action, ​Fewer drug interactions​.
(Lexapro®) Shorter Duration of action, ​Sedation​, C​ I in Prego​→cardiac defects.
Vortioxetine (Brintellix®) Good drug to start with. ​Well tolerated​. Little effect on CYP2D6=​few Drug interactions​.
Vilazodone (Viibryd®) Fewer sexual sfx?

SNRIs Inhibit reuptake of ​both​ ​Serotonin ​and​ NE​. may act quicker. Also used for Neuropathic Pain.
Venlafaxine ​(Effexor®) Hot Flashes
Desvenlafaxine ​(Pritiq) Sfx- ​INC BP​!!!​ SIADH.
Duloxetine ​(Cymbalta) Improves physical ss of depression, to ​tx chronic pain​/fibromyalgia, can cause urinary
Milnacipran​ (Savella) retention, ​CI in 3rd trimester​ & anyone w ​LIVER​ ​dz
Levomilnacipran For Fibromyalgia​. ​For Major Depressive disorder​.
(Fetzima)

Bupropion Inhibits reuptake of Dopamine​ & NE. ​Reduces Cravings​. Good for pts who haven't
(Wellbutrin®) responded well to other drugs. ​Weight loss​!
Sfx- ​anxiety​, wt loss, ​lowers s
​ eizure​ ​threshold​.

Mirtazapine Blocks presynaptic ​α2​ receptors ​(normally inhibit release NE/ 5HT)→​↑ release of NE/ 5HT​.
(Remeron®) Sfx- ​sedation​. Inc appetite and w
​ t gain​.

Atomoxetine For ADHD, causes LIVER damage possible.

(Strattera®)

Amoxapine (Asendin®) Some antipsychotic effect.

Trazodone (Desyrel®) Partial 5HT​1A​ agonist and may block 5HT​2A​. Mores so a sleep aid. Insomnia&pain management
Sfx- ​Priapism​-​rare but serious.
“​TraZZZaBONEer​= sleep and erection)

St. John’s Wort For mild depression. Inc sun sn.

Interacts w everything​. Should not be used w MAOIs/SSRIs/TACs/Ldopa or ​Selegiline​→
serotonin synd
Induces CYP450

Serotonin synd Tx w ​cyproheptadine​ ​(serotonin antagonist)

“3As= Activity (hyperreflexia), Autonomic stim (hyperthermia, HTN), Agitation”

SIADH Causes ​Water reabsorptio​n→conc urine→​hyponatremia→swelling in brain​.

Tx- ​restrict fluids

Phenothiazines Used to Tx ​Schizophrenia​. Also for ​Nausea and Vomiting​.

Chlorproma​zine Drugs in this class have varying potency for D2 receptors.
(Thorazine) Anticholinergics have ​dec​ Extrapyramidal symptoms (​EPS​).
Thiorida​zine​ (Mellaril) Sfx- ​anticholinergic, alpha block→ ​postural hypotension & inhibit ejaculation​, mild
Flu​phenazine​ (Prolixin) jaundice, sedation, Dec ​seizure​ threshold, ​may produce retinal deposits, ​Prolactin inc, tardive
Prochlorperazine dyskinesia​. ​NMS-rigid​/ high temp (tx w dantrolene)
(Compazine) Chlorpromazine= most antimuscarinic- less EPS
Trifluoperazine fluphenazine= least antimuscarinic- more EPS
(Stelazine)

Other Selective ​Blockade of D2​ receptors only. Most likely of all antipsychotics to ​cause
Extrapyramidal Symptoms ​(parkinsons like ss).
Antipsychotics
Often taken w Benadryl ​(blocks muscarinic receptors) to dec EPS.
Haloperidol​ (Haldol)
Tx for ​Tourette’s synd​, ​may inc QT interval​.
Thiothixene (Navane)
Pimozide ​(Orap)
Molindone (Moban)
Loxapine (Loxitane)

New-Generation 1st line. Binds ​D4​ receptors and ​5HT​2A​ receptors>>>D2 thus ​Very Low EPS.
Sfx- most likely to cause ​Wt gain​. I​ NC hyperglycemia​→ T2DM
“Atypical”
No agranulocytosis​.
Antipsychotics Now Last resort
Olanzapine​ (Zyprexa) .Inhibits M/H/alpha receptors. Least likely to cause Tardive Dyskinesia.
Risperidone​ (Risperdal) SFX- ​Agranulocytosis​ (​thus req ​wkly blood testing​-$)
Ziprasidone (Geodon) 1st line for Psychosis. LOW EPS.
Clozapine​ (Clozaril) Sfx- Most likely to cause ​Inc QT​, ​inc prolactin​.
Quetiapine​ (Seroquel) CI- Alzheimer's→ death.
Iloperidone (Fanapt) 1st line. ​Does NOT cause Agranulocytosis. Does NOT cause inc prolactin.
Paliperodone (Invega) Used in adjunct to ​tx-resistant ​depression.
Lurasidone (Latuda) Sfx- ​highly ​sedating​, bipolar depression, drowsy, ​wt gain​.
Asenapine (Saphis) Partial​ Agonist ​at D2 & 5HT​1A​ receptors. ​Antagonist​ at 5HT​2A​. Also Blocks alpha/H receptors.
Tx for depression and ​antipsychotic​ .
Aripiprazole​ (Abilify)
Brexpiprazole (Rexulti® Sfx- sedation, ​Diabetes​, Seizures, Dec Motility of Esophagus (​Difficulty Swallowing​)

Mood Stabilizers Use- tx of​ Bipolar Disorder​.

Lithium​ (Eskalith) Pk- mech not well known, Optimal ​conc .6-1.2 mEq/L= ​Narrow Therapeutic window​. Excreted
Divalproex​ (Depakote), by Kidney. LIthium is reabsorbed by the prox tubule in​ kidney and competes w Na ​for
Valproic acid reabsorption. ​Thiazide​ Diuretics dec Clearance of Lithium. ​NSAIDS​ also dec Clearance of
(Depakene) Lithium.
Gabapentin (Neurontin) Sfx- Tremor, Nausea, HA, Dec Thyroid→ ​hypothyroid​, Renal effects= ​DIabetes insipidus​ (can
Carbamazepine be ​tx w amiloride​), ​Wt gain​, ok for prego.
(Tegretol) Extremely toxic​- >2.0=mild (tremor), >2.5=severe (arrhythmias, death), tx toxicity w ​dialysis
Lamotrigine (Lamictal) and saline​.
Topiramate (Topamax) DI- Antidepressants can→ mania in some, ​thiazides, NSAIDS​, Na
Anticonvulsant​! Freq GI probs. Assoc w ​Liver toxicity​.
GI, CNS toxicity, Hypersn rxns, Hematologic effects, Risk Stevens Johnson synd (SJS)-HLA-B
1502
Worst for SJS, does NOT cause wt gain.

GABA-mimetic Agonist ​at ​GABA​B​ receptors​→ ​Hyperpolarizes​ neurons and Inhibits Ca→ ​Inhibits release of
excitatory transmitters​ from presynaptic terminals in both ​brain​ and ​spinal cord​.
​Bac​lofen (Lioresal®)
Used to tx ​chronic spasticity​ and also for severe​ ​b​ac​k pain​.
Pk- Often given ​Intrathecally
Sfx- Drowsy, ​weak​,​ may inc seizure activity.
“​Bac​lofen for​ ​Bac​k pain”

Benzodiazepine Acts on​ GABA​A​→ dec spasticity.

Sfx- significant​ sedation.
​Diazepam (Valium®)
Used as adjunct tx to chronic spasticity.

Spinal cord or Acts as a ​sedative​. ​Anticholinergic​ sfx→ makes is ​hard to pee​.

Can cause ​confusion and transient visual hallucinations.
brain stem
sedatives Metabolized to ​Meprobamate. Has ​addiction potential.
Cyclobenzaprine Induces hepatic microsomal enzymes.
(Flexeril®)
Carisoprodol​ (Soma®)
Metaxalone (Skelaxin®)
Methocarbamol
(Robaxin®)
Orphenadrine (Norflex®)

Others Analogue of Clonidine- ​alpha2​ agonist​→ inhibits pain transmission in dorsal horn.
Tizanidine (Zanaflex®) Use- dec ​chronic /acute muscle spasms​.
Dantrolene (​Dantrium​) Sfx- sedation, may→ postural hypotension.
Onabotulinum Toxin A Used ​as Emergency tx​!!! Affects excitation contraction coupling in muscle, ​Blocks Ca release​.
(​Botox®​) Used to ​tx malignant hyperthermia​.​ & NMS
Blocks​ the release of ​Acetylcholine​. Very ​small​ ​amts​ of botox injected in ​Local​ area.
Used for muscle spasms/ stroke/ sweating/ remove wrinkles.
CNS Stimulants Cause inc ​Euphoria​, alertness, inc energy, ​dec appetite​.
Methylphenidate Pk-​ Inc DA and NE ​in presynaptic terminal.
(​Ritalin®​) Can Cause ​Paranoia​/ Delusions.
Amphetamine (Adderall) High Abuse potential. Withdrawal- not life threatening.
Methamphetamine Meth→ meth Mouth.
Atamoxetine (Strattera) Uses- Narcolepsy (less addicting),​ ​ADHD​, Obesity.
Caffeine Blocks Adenosine→ inc CAMP.

Parkinson’s Dz
Levodopa (​Dopar®​; Ldopa will cross BBB. also metabolized in GI/ peripheral tissues. So only small portion is
Larodopa®) Carbidopa actually getting to brain.
(Lodosyn®)
Now use Combined w ​Carbidopa- a dopa decarboxylase inhibitor​ (cant cross BBB- thus only
Carbidopa/levodopa works in peripheral tissues→ and ​Inc LDopa in brain​.)
(​Sinemet®​) Use- Parkinson's, effect will dec w time as neurons dec.
Sfx- ​Nausea and Vomiting​. H ​ TN​ when combined ​w MAOIs​.
When ​Dyskinesias​ start happening=time to switch to new drug.
If Psychosis- tx w atypical antipsychotics (clozapine/Quetiapine/Aripiprazole= lower D2 blocking)
DI- ​MAOIs→ HTN​, Pyridoxine (VIT B6)
CI- ​Psychosis, Closed angle glaucoma, cardiac dz, active peptic ulcer, malignant melanoma.​

Selegiline (​deprenyl; Inhibits ​MAO-B​ ​(predominant form in striatum→ dec striatal metabolism of dopamine).
Eldepryl; ​transdermal SFx: ​Insomnia
patch:​ ​ ​Emsam®) DI- ​Do NOT combine w ​Meperidine​.
Rasagiline​ (​Azilect®​) Irreversible MAO-B inhibitor. Less Insomnia.
Entacapone​ (Comtan; COMT ​inhibitors, adjunct tx w Ldopa/carbidopa tx to dec breakdown, can cause
with l-dopa/carbidopa, Rhabdomyolysis.
Stalevo)

Bromocriptine An ​Ergot​ derivative​, D2 agonist→ ​Dec release of prolactin.

(Parlodel) Sfx- anorexia, nausea, vomiting, Postural hypotension, Arrhythmias, ​Erythromelalgia​ (Red
Prami​pex​ole​ (Mirapex) hands and feet​). ​“​Bro​ got caught ​red handed​”
Ropin​irole​ (Requip®) Not an Ergot, sfx- ​Sudden sleep​ during day.
Rotigotine (Neupro®) For ​restless leg synd​.
Apomorphine​ (Apokyn®) Fast onset, short half-life. Temporary Rescue of on/off periods

Amantadine Antiviral for flu used for Parkinsons to​ increase Dopamine Synthesis/release/reuptake.
(Symmetrel®) OD→ Toxic psychosis/convulsions.
SFx: ​Livedo Reticularis (Spotting of skin)​. Peripheral edema.
Can be used to tx parkinson's but not very effective.

Benztropine Anticholinergic​ → dec acetylcholine. Helps ​improve rigidity/tremor.

(Cogentin®) Discontinue gradually! (Benadryl)
Biperiden (Akineton®)
Alzheimer’s Disease

Donepezil ​(Aricept®) Inhibit breakdown of released acetylcholine. Improve ss for a while until loss of nerves.
Rivastigmine (Exelon) Sfx- ​GI overactivity
Galantamine (Reminyl)

Memantine (Ebixa®; Blocks NMDA receptor. ​Renal excretion!!!- (carefully watch)

Namenda®)

Pharmacogenetic Receptor polymorphisms- glucocorticoid, androgen, estrogen, potassium channels, sulfa

receptors.
s
Drug transporters- OATP1B1
Most likely cause of a genetic mut is the ​SNPs

Isoniazid Gain of Function, ​N-acetyltransferase ​2 gene (​NAT2​).

Slow acetylators - Isoniazid, ​Procainamide, hydralazine​→ Lupus
Fast Acetylators- Isoniazid→ ​Hepatotoxicity​.

Codeine Change in​ Gene Copy ​Number​. ​CYP2D6​.

Nortriptyline Involved in the​ metabolism of- Codeine, Nortriptyline, Debrisoquin.
Debrisoquin CYP2D6 has over 90 alleles​→ poor metabolizers, Intermediate, extensive and Ultrarapid
metabolizers. ​Will affect ​Optimal Dose.

Abacavir HLA-B​ 5701- ​hypersensitivity reactions​ (​Stevens Johnson Synd)