Med Chem E4 distintive properties

Which is the most potent and least potent Volatile Liquid anesthetics? What are other properties of that?

Most—> Halothane bc low MAC(0.74%)

Least—> Desflurane bc HIGH MAC(6%)

• makes it the safest too—> does cause irritation to airways tho

• lowest bP too

Which Volatile Liquid anesthetics is widely used and has a pungent smell?

Isoflurane

Which Volatile Liquid anesthetics is not used anymore?

Halothane(metab in to acid, CV and kidney effects) and Enflurane(high metab rate and side effects)

Which Volatile Liquid anesthetics has the fastest onset?

Sevoflurane @ 1-2 min

desflurane—> 2-3 min and enflurane and iso—> 7-10min

Advantages of intravenous injections

• No special equipment needed to administer

• Many have faster onset than inhaled agents

• Rapid recovery; suitable for outpatients

Which intravenous injections are schedule 3 controls?

Ketamine(causes hallucinations)

Esketamine

Thiopental Sodium

Which intravenous injections are schedule 4 control?

Fospropofol, Midazolam, Remimazolam, Methohexital,

Which intravenous injections is a NMDA receptor antagonist and allosteric antagonist?

Ketamine HCl

• S- enantiomers more potent, but racemix admin

• also has active metabolites

How are ketamine and esketamine different?

Ketamine- racemix, IV

Esketamine- just S ent, NASAL SPRAY(under clinical supervision)

Which intravenous injections is widely used and drug of choice for ambulatory surgery? What is it used for?

Propofol→ used for induction, maintenance or sedation IN ICU; anti-emetic

• EMULSION(white and milky)

• inactive metabolites

• ADRs: microbial growth, pain @ injection, allergy

• increases GABA

Fospropofol: the PRODRUG for it (not used widely)

Which intravenous injections enhance GABA binding @ GABA receptor A? Whats the difference between them? Similarities

Midazolam

• for pre-op, causes amnesia, might need other drugs to wake pts up,

Remimazolam

• soft drug; short duration, ultra fast acting; faster recovery time

Similarities

• YES smooth muscle relax, benzodiapines, higher CNS depression

Etomidate chiral center, and used for what?

ONLY R ent ; used to induce anestheria but NOT analgesia

• NOT A CONTROL

• no muscle relax

Which intravenous injections are barbiturates? How are the different? How are they similar?

Methohexital:

• unsaturated substituent, racemix

Thiopental

• saturated substituent, more lipophillic(enter CNS quick and leave quick too)

• active metabolites(removing sulfur), drug accumulation, NOT used in CNS anymore(used in deathrow)

Similarities:

• ultra short acting, short duration of action

Barbiturates classifications and drugs in it

Ultra short(<3hr)- Methohexital and Thiopental

Short(3-4hr)- Secobarbital and Pentobarbital

Intermediate(6-8hr)- Amobarbital, Butabarbital

Long(10-16hr)- Phenobarbital

Barbiturates schedule 2 drugs

secobarbital, pentobarbital, amobarbital

Barbiturates schedule 3 drugs

thiopental, butabarbital

Barbiturates schedule 4 drugs? what is it used as?

phenobarbital; used as an anti-consulvant and for grand-mal seizures

S> R metabolite; oxidative hydroxylation and glucoronidation

How is secobarbital metbolized? What about amobarbital?

seco: a-oxidation, epoxidation which inactivates P450, and w-1 oxidation

amo: w/w-1 oxidation

How are all barbituates used?

as sedative and hypnotics;

Which drug is given with fruit juice to hid the bitter taste? What control is it, whats the metabolism and what ADRs? What metabolites are active?

Chloral Hydrate

• safe for children but can cause GI irritation

• favors hydrated form

• schedule 4 control

• oxidation to ketone; reduction to alcohol which is active

What are the Z drugs and what control are they? What are they used for?

Zolpidem, Zaleplon, Eszopiclone

all are control 4 drugs

used for insomnia; zolpidem for military too.

Which Z drug is extensively metabolized?

Zolpidem- major is COOH all is inactive metabolites tho

Which Z drug is S ent. more prevelant?

Eszopiclone

Which drug is a selective alpha 2 AGONIST that is used as a sedative in ICU for intubating or ventilating?

Dexmedetomidine

• regional or anginal anesthesia

• IV or buccual or Sublingual

• major metabolite is oxidation

• decreases NE—> CNS depression

Which drug mimics melatonin and is approved for long term insomina because it is a sleeping aid without abuse or withdrawal symptoms?

Ramelteon

• binds to MT1 AND MT2 receptors

• use S ent

• has active metabolite; but first pass is very oof

• DDI with fluvoxamine

Which drug mimics melatonin but has a conformation restriction and is used in BLIND ppl.

Tasimelteon

• higher MT2 affinity for circadian rythm

• used for non-24 hours sleep wake disorder(blind ppl) and nightime sleep disturbance and MAGNESIS syndrome

• metabolism is hydroxylation of benzne ring

DORA drugs information. Which is the longest half life?

• dual oxrein A and B neuropeptides; work on OX1R and OX2R receptors

• food delays onset so take 30 min before bed time

• helps sleep for more than 7 hrs

• second line treatments

Lemborexant is longest t/2

What controls are benzodiazepines?

Schedule 4

Which benzodiazepines have lots of generics?

Cholordiazepoxide HCl

• has active metabolites

• NOT a prodrug

What drug has the metablites temazepam and oxazepam? What are the metabolites used for?

Diazepam

• active metabolites(nordiazepam w demethylation)

• anxiety relief

• yes musle relax

Tema: hypnotic

Oxa: anxiety + alc withrdwal; used for liver dysfunction in elderly

Which benzodiazepines is used for epilepsy and is a prodrug?

Clorazepate Dipotassium- also alc withdrawl

metabolite has 36-100hr t/2

Which benzodiazepine is used for sleep inducing activity and is a prodrug? Which benzodiazepine shares the same metabolite as this?

Flurazepam; sedative and hypnotic thru REM cycle

major metabolite is long lasting, minor is thru deamination

same metabolite as Quazepam→ active metabolites for insomina.

Which benzodiazepine is used for seziures?

Lorazepam- also used for SEVERE withdrawal symptoms and is the treatment of choice for delirum tremens

• also fo anxiety and anticonsulvants

Triazolobenzodiazipines potentcy from most to least? What is each of their indications?

Triazolam» Alprazolam» Estazolam

Triazolam→ agorophobia, anxiety and panic disorder

Alprazolam→ insomnia and sleep

Estazolam→ rebound insomnia and sleep

all have hydroxylation of phenyl ring as metabolism

Which drug is benzodiazepine receptor antagonist? what does it treat, and what does it do? what side effect does it have? How is it metabolized?

Flumazenil—> REMOVES CNS effect; SOFT DRUG, treats reocurent symptoms, and reverses benzodiazipine overdose.

side effect: seizures

metabolism: deactivated thu ester hydrolysis

IV

Which drug is a full and partial 5HT1A receptor agonist?

Buspirone

• D2 agonist too

• “clean drug“

• 1-PP metabolite like Geprione thru cleavage

Which drug is a 5HT1A partial agonist and indicated for MDD?

Gepirone → tested for anxiety but NOT approved

1-PP metabolite like busprione

presynaptic controls of NE

What is 1-PP metabolite? What drugs is it s metabolite of?

alpha 2 antagonist

Gepirone and Buspirone

Which anxiolytic agent is a 1st gen antihistamine?

Hydroxyzine

• mild tranquiler for anxiety reduction

• birth defects

Which drug is known as the “happy pill?”

Meprobamate - used for anxiety;

• schedule 4 control

• barbituate like activity at GABA A receptor

• w-1 on alkyl chain metabolism

What drug is used for the neuromuscular aspects of tetanus?

Methocarbomal

• need to combo with analgesic

• and relives discomfort with

Which skeletal muscle relaxant is control drug?

Carisoprodol- schedule 4

• racemix

• 2 metabolite=> meprobromate

• spinal cord, no muscle

Which skeletal muscle relaxant is a GABA deactivator and GABA B receptor agonist?

Baclofen

• racemix

• used as a sleeping pull, muscle splacity from MS and trauma in spinal cord

• DOESNT reduce muscle strength

• no oxidation; little metabolism

Which skeletal muscle relaxant has Amrix as the ER formulation, with all other brands being discontinued?

Cyclobenzaprine

• active metabolites bc demethylation

• glucoronidation—> epoxide which is inactive

Which drug is a Ry receptor antagonist and used as IV first?

Dantrolene

• for malignant hypothermia, stroke, cerebral paslay, direct muscle effect

• inhibits Ca++ release; causes hepatox

• IV first and then oral maintenance

• carcinogen

Which skeletal muscle relaxants have anticholinergic effects?

Orphenadrine

• causes drowsiness

• treats leg cramps and relives pain from discomfort

Which skeletal muscle relaxant lowers blood pressure and is used for acute and intermittent muscle spasitaity

Tizadine

• alpha 2 agonist

• extensively metabolized

Which are the alphatic phenothiazines? What is similar? What is differenent?

Chlorpromazine, Triflupromazine, Promethazine

• protect ALL from light- blue containers to prevent oxidation

Chlorpromazine→ D2 antagonist, and 7-hydroxy metabolite; sulfone/sulfaxide which are inactive metabolites

Triflupromazine→ increase lipo

Promethazine→ weak antipsychotic; controls motion sickess and post op; antihistamine and antiemetic

Which drug is a piperdine phenothiazine?

Thioridazine→ weak antipsychotic

oxidation to sulfoxide then sulfone by CYP2D6

• active!!; sulfone is discontinued tho bc CV and QT prolong

• active metabolites have more activity

Which antipyschotics are classified as piperazine phenothiazines? Whats the same? Whats different?

Trifluroperazine

• antiemetic but not used for it, MORE POTENT, used for short term anxiety

Prochloroperazine

• used for nausea and vomitting, antipsychotic

Both:

• schizo and antipyschotic

Which antipsychotics are piperazineethanol phenzothiazine?

Perphanazine(IV) and Fluphenazine(oral or IV)

Fluphenazine

• multiple times admin at low doses

• Enanthate—> every 2 wks

• Decaoate→ once 3-4 wks

• both are Subq or IM, hydrophobic and slowly released

  • also oil suspension for schizo

Which antipsychotics is a isosteric phenothiazine and the Z ent is more active?

Thiothixene

• D2 receptor + serotonin and histamine receptor too

Which antipshycotic is an indole and is discontinued?

Molindone Hcl

• D2 antagonist

Butyrphenones. How are the similar? Different

Haloperidole→ used for schizo, tourettes

• d2 inverse agonist, increases cyclic AMP; multiple admin oral or IV

• in seasame oil formulation for IM q4wks

• hydroxy conjugation major metabolite

Droperidole

• NO antiphyscotic activity, serotonin and dopa activity

• doe reduction of n/v post ops or diagnosis treatment; IV for chemo vomiting

• extensive metab

Pimozide

• extensively metabolized, supresses ticks, NOT antipyschotic, mutliple times day admin

Which inorganic drugs are used for bipolar disorder?

Lithium Carbonate and Citrate

• inhibits sodium reabsorption→ sodium defiency(urine elim)

• increase NE uptake

Which typical antipsychotics causes extra pryimidal symptoms?

Loxapine succinate

• causes EPS like tardine diskenia

• 1st gen

Which drug has the lowest risk of EPS symptoms?

Clozapine

• risk of agranulacytosis tho

Which drug has oral tablets, oral solution, ODT, polymer formulation, long acting injection forms?

Riperidone→ benzoisoxazole

tabs/solution/ODT→ mutiple doses

active metabolite called Paliperiodne which has hard shell(ER form) (INVEGA)

• monthly→ sustema; 3 months→ Trinza; 6 months→ Hafyera

polymer→ Consta→ IM in polymer matrix; 2wks dosing

Which second gen antipsychotics has 5HT3 serotonin antag and 5HT1 agonist and has food effects?

Zipasidone/Lurasidone

• increases absorption w food

• for schizo and bipolar

• treats + and - of schizo

Which 2nd gen antipsychotics has NO agranularcytosis risk and is similar to clozapine?

Olanzapine

• less eps

• bipolar and schizo and lil sedation

Which drug has a thiazepine, and has seratonin and dopa antagonism? (antipsychotics)

Quetiapine Fumarate

• atypical→ ± symptoms

• oxidized by air to sulfoxidel alc-cooh(inactive)

Which 2nd gen antipsychotics has partial agonist at D2 and 5HT1A and antagonist at 5HT2A?

Aripiprazole

• ER long acting formulation→Abilify Maintena; IM; micropartical suspension

• prodrug→ Aripiprazole lauroxil(Astrida)

  • emulsion;

  • ester hydolysis

• for schizo, MDD, tourettes

Which 2nd gen antipsychotics is for agitation in alzheimer’s?

Brexpiprazole

• MDD, schizo too

• high F- 95

Which 2nd gen antipsychotics has no generic and contains urea?

Cariprazine

• active metabolites by N deaklyation

• long t/2→ 2-4 days

• schizo, MDD, bipolar

• 5HT2A/B antagonist

Which drug is admin sublingual and is a mix of 2 isomers?

Asenapine

• treats bipolar disorder and schizo

• avoids first pass

Which 2nd gen antipsychotics should u avoid grapefruit juice with and is a butyrphenone?

Lumateperone

• 5ht2a antagonist; dopa too

• CYP3A4 to 20+ metabolites

Which new antiphycotics is a mix of 2 drugs? Which stays in peripheral and which goes CNS?

Xanomeline and Trospium

Xanomeline

• M1,4 Agonist

  • m1→ improves cog func and negative schizo aspects

  • m4→decreases NE, positive schizo

  • GI and CV side effects

Trospium

• mimics acoa; musciarinic receptor ANTAGONIST; stays in periphery

treats schizo, oral

Which drugs are succinimides for petit mal seizures? What are similarities and differences?

Ethosuximide: skin issues, longer t/2

Methsuximide: side effects, fetal issues

Both: monitor blood counts, urniary analysis, liver func

Which drug is an oxazolidinedione that is toxic to the blood, skin, and fetus?

Trimethadione

• last resort

• active metabolite thru demethylation

Which petit mal drug is used with a sodium salt form 1:1?

Valproic Acid

• petit mal, seizure partial, bipolar

• omega and beta oxidation

• BBW: tetratogenicty and pancreasitis(fatal)

Which petit mal drug can be used for glaucoma and acute mountain sickness but also cause kidney stones?

Acetazolamide

• carbonic anhydrase inhibitor → increse urine pH

• decreases HCO3 conc in eye too→ decrease pressure

• cystiene buildup→ kidney stones

Which isosteric barbiturates and have 2 metabolites?

Primidone

• not a prodrug

• major metab→ cleaved at the top(diamide)

• grand mal seizures

Which partial/grand mal seizure drugs is also used for status eplietilus, or seizures during neurosurgery?

Phenytoin Sodium

• hydroxylation to S ent; injecton are painful

Which grand mal seizure drug is a injectable prodrug?

Fosphenytoin Sodium,

• status epliticous and sezires during neurosurgery

Which dibenzazepines can induce it’s OWN metabolism?

Carbamazepine

• grand mal/partial seizures NOT petit + bipolar disorder

• CYP3A4 to epoxide which is active/ diol is inactive

• can agranularcytosis and aplasticanemia

Which drug has a 6 carbon sugar and treats partial/grand mal seizures?

Topiramate,

• potentiate GABA binding

• unchanged elim

Which drug treats partial/grand mal seizures and is a AMPA antagonist?

Perampanel

• 4yo> partial

• 12> grand mal

• oxidative metab

• not binding to glutamate site

Which drug treats partial/grand mal seizures and has amino acid(D-serine) embedded into it?

Lacosamide

• high F→ BID dosing

• urine elim, 40% unchanged

Which drug for partial seizure inhibits GABA resulting in more staying at the synapse?

Tiagabine → extensive metab

Which drug for partial seizure is a GABA derivative and has a saturation effect?

Gabapentin

• for post heptatic neurolgia, neuropatic pain, restless leg syndrome

• prodrug created for this-> gabapentin enacarbril-> horizent

  - start with cleaving ester bond; casacade prodrug

Which drug for partial seizure is 3d printed and works on SV2A? Which has a similar metabolism to this?

Levetiracetam

• inhibits Ca++ channels→ reduce neurotransmitter release

• IV oral admin

simiar: Brivaracetam

Which drug for partial seizure is an K+ channel openner and an adjunt?

Ezogabine/retigabine

• extensive metabolism

Which drug is used in tuberculosis which is caused by epilepsy in childhood?

Cannabidiol

• + duvette syndrome and lennox gastro syndrome

Which drug is used in eclampsia via IV or IM?

Magnesium Sulfate

• CNS depressant

Which drug treats huntington’s disease and tourettes?

Deutetrabenazine

• active metabolite (ketone→ alcohol)

• also for tardine dyskinesia

Which drug is used for tardine dyskinesia and is a prodrug?

Valbenazine

• ester hydrolyzed