PHARMACOLOGY II – BLOCK 2:

  1. Mood Drugs
  2. Anxiety Drugs
  3. Epilepsy Drugs
  4. Neuropathic Pain Drugs
  5. Migraine Drugs
  6. ADHD Drugs
  7. Alzheimer Drugs
  8. Parkinson Drugs
  9. Huntington Drugs
  10. Drugs of Abuse
  11. Schizophrenia Drugs
  12. Block 2 Prep Questions

Disclaimer: These notes do not cover all the drugs for block 2, specifically the drugs for Asthma, COPD, Serotonin drugs, Antihistamines, Prostaglandin, Pulmonary Hypertension, Emetics/Antiemetics, Peptic Ulcers, GERD, Lower GI, IBD, Anemias, Glaucoma, Metal poisonings, or Local Anaesthetics.

Highlight using your mouse to view the answers.

MOOD DRUGS

Q: How long does it typically take an antidepressant drug to have a meaningful effect?
A: 3-4 weeks

Q: How long does it take lithium to work?
A: 14 days

Q: What are the four main classes of antidepressants?
A: Monoamine Oxidase Inhibitors (MAOI), Tricyclic Antidepressants (TCA), Selective Serotonin Reuptake Inhibitors (SSRI), and Serotonin Norepinephrine Reuptake Inhibitors (SNRI).

Q: What are the three main neurotransmitters involved in mood?
A: Norepinephrine (NE), Serotonin (5HT), Dopamine (DA) — they are the monoamines, inhibited by MAO

Q: Which MAOI is used for Parkinson Disease?
A: Selegiline. So you can treat Parkinson with Trihexybenzamine, Benztropine, and Selegiline.

Q: How do you abbreviate these:
A: one per day — QD (quaque diem)
two per day — BID (bis in diem)
three per day — TID (ter in diem)
four per day — QID (quarter in diem)

Q: What are the four major MAOI drugs?
A: Isocarboxazid, Phenelzine, Tranylcypromine, Selegiline (remember Phen, Tran, the Giline’s, and the Isolated communists are MAOists)

Q: What mood drug classes have the adverse effects of orthostatic hypotension, lowers seizure threshold, and induces mania/hypomania?
A: MAOI, TCA

Q: What mood drug classes have the adverse effects of lowering seizure threshold and induces mania/hypomania but does NOT cause orthostatic hypotension?
A: SSRI, SNRI

Q: What mood drug class causes hypertensive crises due to the “cheese effect” when you ingest it with tyramine-containing foods?
A: MAOI

Q: What mood drug class also has H1 and M1 antagonism, leading to sedation (from H1 antagonism), weight gain (from H1 antagonism), and anticholinergic effects (from M1 antagonism)?
A: TCA

Q: What mood drug class can cause serotonin syndrome (increased muscle tone, agitation, hyperreflexia, increased temperature)?
A: SSRI

Q: What is the most major adverse effect of SSRI?
A: Sexual dysfunction

Q: Which mood drug class can give you nausea, dizziness, and headache after you stop using it for 1-3 days?
A: SSRI — this is called SSRI Discontinuation Syndrome

Q: What mood drug has significantly less side effects than the main mood drugs, but does lower seizure threshold and does not cause sedation, cardiovascular effects, anticholinergic effects, “switching” to mania/hypomania, or sexual dysfunction?
A: Bupropion

Q: What are the side effects of bupropion?
A: Remember, bupropion has very little side effects, but it does lower seizure threshold (dose related), decreases appetite, and cause agitation.

Q: What mood drug has significantly less side effects than the main mood drugs, but does NOT lower seizure threshold, but DOES cause sedation?
A: Mirtazapine

Q: How long do you have to wait between taking MAOI and SSRI/SNRI/TCA/Bupropion?
A: 14 days

Q: How long after taking fluoxetine can you take a MAOI?
A: 5 weeks

Q: What is the mechanism of action for TCAs?
A: inhibit reuptake of 5-HT and NE (like SNRI) at presynaptic neuron.

Q: What TCA do you use to treat Obsessive Compulsive Disorder?
A: Clomipramine (“clone my pralines”)

Q: What TCA do you use to treat Panic Disorder?
A: Imipramine (“I’m a’panicking”)

Q: What are the five common TCA’s covered in lecture?
A: Clomipramine, Amitriptyline, Nortriptyline, Desipramine, Imipramine (“TCA CANDI”)

Q: Desipramine is the active metabolite of what, and therefore has less sedation/anticholinergic/hypotension side effects?
A: Imipramine (“Imi becomes Desi”)

Q: Nortriptyline is the active metabolite of what, and therefore has less sedation/anticholinergic/hypotension side effects?
A: Amitriptyline (“Ami becomes Nora”)

Q: All SSRI drugs inhibit CYP2D6 except which one?
A: Fluvoxamine

Q: What drugs are metabolized by CYP2D6?
A: Atomoxetine, Risperidone, TCA!!!, Aripiprazole

Q: Why do SSRIs increase TCA levels?
A: Because SSRIs inhibit CYP2D6, which normally metabolizes TCA. Therefore you can’t metabolize TCA, and so TCA levels rise.

Q: How do SSRIs work?
A: inhibit reuptake of Serotonin (selective serotonin reuptake inhibitor)

Q: Can you use MAOIs concomitantly?
A: NO!

Q: Why don’t you use SSRIs and MAOIs and other serotoninergic drugs together?
A: Because it will increase 5-HT too much and cause Serotonin Syndrome (increased muscle tone, agitation, hyperreflexia, increased temperature, arrhythmia, death)

Q: What are the six SSRIs we learned in class?
A: Fluoxetine, Fluvoxamine, Sertraline, Paroxetine, Citalopram, Escitalopram (“Flu-Flu, Ser-Par, Cit-Escit”)

Q: What’s the MOA for SNRIs?
A: block reuptake of serotonin and norepinephrine

Q: What are the three big SNRIs we covered in class?
A: Venlafaxine, Desvenlafaxine, Duloxetine (“Saturday Night DVD”)

Q: Which SNRI can also block reuptake of DA?
A: Venlafaxine (“SDNRI”)

Q: The adverse effect of venlafaxine looks just like SNRI except what difference?
A: No tremors with venlafaxine

Q: Desvenlafaxine is the active metabolite of what?
A: Venlafaxine

Q: What is venlafaxine used for?
A: General Anxiety Disorder, Social Anxiety Disorder (“Gundi and Benji’s Drug”)

Q: What unique thing is duloxetine used for?
A: control the pain from diabetic peripheral neuropathy

Q: Besides the four main classes of antidepressants (MAOI, TCA, SSRI, SNRI), what are the three “Other Antidepressants” we covered in class?
A: Bupropion, Mirtazepine, Trazodone

Q: What’s the MOA for Bupropion?
A: inhibit reuptake of NE and DA (“NE/DA RI”)

Q: What is Bupropion used for?
A: Smoking cessation, ADHD

Q: What’s the MOA for Mirtazapine?
A: Alpha-2 antagonist –> increased NE and 5HT. Also antagonizes H1 –> causes sedation.

Q: What’s the MOA for Trazodone?
A: Two things: 1. blocks 5HT reuptake and also acts as a 5HT agonist. 2. Blocks presynaptic alpha-2 and post-synaptic alpha-1, causing orthostatic hypotension.

Q: What’s the active metabolite of Trazodone that acts as a 5HT agonist?
A: m-CPP (m-chlorophenyl piperazine)

Q: Most antidepressants can cause suicidal behavior in kids. What are the only two antidepressants that are approved in children?
A: Fluoxetine and Escitalopram

BIPOLAR DRUGS

Q: What three classes of drugs do you use to treat bipolar disorder?
A: Mood stabilizers (i.e. lithium, valproic acid, carbamazepine, lamotragine, other antiepileptic drugs), Antidepressants, and Antipsychotics.

Q: What drugs do you use to treat the depression part of bipolar disorder?
A: Antidepressants

Q: What drugs do you use to treat the mania part of bipolar disorder (for both acute and prophylaxis/maintenance)?
A: Mood stabilizers and Antipsychotic drugs

Q: What drugs do you use to maintain or prevent (prophylaxis) bipolar disorder episodes?
A: Mood stabilizers (including Lamotragine)

Q: What antidepressant drug has less risk of antidepressant-induced mania/hypomania and therefore is better for bipolar disorder?
A: Bupropion

Q: What are the adverse effects of lithium?
A: GI irritation, tremor, metallic taste, COGNITIVE DULLING. When used long term, like for maintenance, can also cause weight gain, acne, polydipsia/polyuria/nephrogenic diabetes insipidus, hypothyroidism.

Q: Lithium Toxicity can occur with serum levels above what?
A: above 1.5 mEq/L —- TEST QUESTION!!!

Q: What two special adverse effect does Carbamazepine cause?
A: Steven Johnson Syndrome (“Steve likes carbs and lambs” — carbamazepine and lamotragine both can cause SJS). Also can cause agranulocytosis, so need to monitor WBC.

Q: What’s unique about the metabolism of Carbamazepine?
A: It induces its own metabolism (within 4-8 weeks) because it induces CYP450 but also gets metabolized by CYP450. So you have to constantly monitor and adjust its level. Because it induces CYP450, it also reduces the levels of oral contraceptives.

Q: Why do you ask a bipolar patient if they are taking oral contraceptives?
A: Because carbamazepine induces CYP450, which metabolizes oral contraceptives. Prescribe something else if they are taking oral contraceptives.

Q: What’s the MOA of Carbamazepine?
A: increase the inactivation of Na channels (“salt granules, fennel, and lambs flying through a maze of pine trees” — Phenytoin, Carbamazepine, and Lamotrigine all work by inactivating Na channels)

Q: What’s the MOA of valproic acid?
A: decrease GABA transaminase, preventing GABA from breaking down. Valproic Acid also decreases sodium and calcium channels. (“VV no GABA T” — valproic acid and vigabatrin both decrease GABA transaminase)

Q: What’s the major adverse effect of valproic acid?
A: Hair loss

Q: What’s the MOA for lamotrigine?
A: inhibits glutamate release, inhibiting sodium channel.

Q: What are the major adverse effects of lamotrigine?
A: SJS (Steven Johnson syndrome) and TEN (toxic epidermal necrolysis)

ANXIETY DRUGS

Q: What classes of drugs can you use to treat Anxiety?
A: Antidepressants, Benzodiazepines (if rapid effect needed, like in panic attacks), and two others (buspirone and clonidine)

Q: How long does it take benzodiazepines to work?
A: 30 minutes to an hour (vs. antidepressants, which take 3-4 weeks). Therefore it is used in panic attacks that occur all of a sudden.

Q: What neurotransmitter is implicated in anxiety?
A: Too little GABA

Q: This isn’t on the test, but what is the generic name for Xanax?
A: Alprazolam (a benzodiazepine)

Q: What are the adverse effects of benzodiazepines?
A: Sedation, DEPENDENCE (so it can be abused), Withdrawal syndrome, Potentiation of alcohol (because binds to same chloride channel as benzodiazepine).

Q: What can you use to treat OCD?
A: Clomipramine, and the SSRIs (flu flu ser par cit escit)

Q: What are the high potency benzodiazepines that can be used to treat anxiety and panic?
A: Alprazolam and Clonazepam.

Q: What’s the difference between the MOA of benzodiazepines vs. barbiturates?
A: benzodiazepines increase FREQUENCY of Cl ion channel opening at GABA-A receptor, whereas barbiturates increase DURATION.

Q: Why is alcohol a depressant?
A: Because like benzodiazepines and barbiturates and GABA, it binds to the chloride channel and hyperpolarizes the neuron (remember Physio I?)

Q: What can you use to treat alcohol withdrawal?
A: Benzodiazepine, because it binds to same chloride channel as alcohol.

Q: What is the most important adverse effect of benzodiazepine?
A: Sedation (like TCAs, therefore used in hypnotics), Dependence, Withdrawal (anxiety, myoclonic jerks, seizures)

Q: Why do you have to be careful when giving benzodiazepines and digoxin together?
A: because benzodiazepines increase the half life of digoxin

Q: What drug is a benzodiazepine antagonist?
A: Flumazenil — reverses the action of benzodiazepines at the benzodiazepine receptor only (not EtOH or barbiturate receptors). Used in reversing benzodiazepine sedation or overdose.

Q: What is the MOA for buspirone?
A: 5HT1A full agonist presynaptically, and partial agonist postsynaptically. Therefore it decreases 5HT synthesis and therefore decreases neuronal firing, treating anxiety.

Q: What’s so good about buspirone vs benzodiazepines for treating anxiety?
A: buspirone has no sedation, abuse potential… therefore good for ELDERLY and patients with medical conditions!

Q: What can you give to improve sexual function in patients taking SSRI?
A: buspirone, because it decreases 5HT, counteracting SSRI, which increases 5HT.

Q: What is the MOA for clonidine?
A: It is an alpha-2 agonist, decreasing the release of the NE.

EPILEPSY DRUGS

Q: What are the six conventional anti-epileptic drugs we covered in lecture?
A: Carbamazepine, Phenytoin, Valproic Acid, Phenobarbitol, Primadone, Ethosuxamide

Q: What are the new anti-epileptic drugs we covered in lecture?
A: Gabapentin, Lamotrigine, Levetiracetam, Tiagabine, Topiramate, Zonisamide, Lacosamide, Pregabalin, Vigabatrine, Felbamate

Q: What conventional anti-epileptic drug treats all partial seizures (simple, complex, secondarily generalized), in addition to generalized tonic-clonic seizures (which all conventional AEDs treat)?
A: Carbamazepine, Phenytoin, Valproic Acid

Q: Which conventional anti-epileptic drug treats secondarily generalized Partial seizures only, in addition to generalized tonic-clonic seizures (which all conventional AEDs treat)?
A: Phenobarbital, Primidone

Q: Which conventional anti-epileptic drug treats all partial seizure types and all generalized seizure types?
A: Valproic acid

Q: Which conventional anti-epileptic drug treats absence seizures only?
A: Ethosuxamide

Q:All of the newer AEDs treat all the partial seizure types, but only one also treats all generalized seizure types. What is it?
A: Lamotrigine

Q: Which drugs treat Lennox-Gastaut Syndrome (seizures in kids + MR)?
A: Lamotragine, Topiramate, Felbamate, Rufinamide (“top lamb felt rough”)

Q: What deficiencies can be caused by phenytoin?
A: Folate and Vitamin D deficiencies

Q: What other adverse effects do phenytoin cause?
A: gingival hypertrophy, blurry vision

Q: When you hear “3-Hz spike-waves” what should you think of?
A: Absence seizures

Q: How do Phenytoin, Carbamazepine, and Lamotrigine work?
A: by prolonging recovery from inactivation of Na channels

Q: What are two adverse effects of carbamazepine?
A: Agranulocytosis and Steven Johnson Syndrome (remember Steve likes carbs and lambs)

Q: What seizure drugs can cause diplopia?
A: Phenytoin, Lamotragine, Gabapentin, Carbamazepine.

Q: What class of antiepileptic drugs can cause porphyria as an adverse effect?
A: Barbiturates (phenobarbitol, Primadone)

Q: What are the three unique adverse effects of valproic acid?
A: hair loss, hepatotoxicity, weight gain. you also get abdominal pain but that ain’t that unique.

Q: What is the adverse effect of ethosuxamide?
A: aplastic anemia (ethosuxamide sux), Steven Johnson Syndrome (extra sux).

Q: Why isn’t felbamate used anymore?
A: Because it cases aplastic anemia and hepatic failure

Q: How does gabapentin work?
A: by increasing GABA

Q: How does tiagabine work?
A: It inhibits GABA transporter (GAT-1), and so it GABA stays put longer.

Q: What is the MOA for Pregabalin, Gabapentin, Ethosuxamide, and Zonisamide?
A: decrease calcium channel currents. Ethosuxamide and Zonisamide decrease T-type (transient) currents. Gabapentin decreases L-type (long-term) currents.

Q: What is the special adverse effect of zonisamide?
A: renal calculi

Q: What is zonisamide used for?
A: adjunctive therapy for partial seizures

Q: What is the MOA for valproic acid and vigabatrin?
A: they decrease GABA transaminase, which increases GABA. Valproic acid also decreases Na and Ca channels.

Q: What is the adverse effect of topiramate?
A: acute closed-angle glaucoma (like atomoxetine for ADHD Rx)

Q: What is the adverse effect of vigabatrin?
A: severe peripheral visual field defects!!

Q: What treats status epilepticus (seizures longer than 30 minutes)?
A: Benzodiazepines

NEUROPATHIC PAIN DRUGS

Q: What two antidepressants can you use to treat neuropathic pain?
A: TCA, SNRI — both increase NE and 5HT

Q: What three antiepileptic drugs can treat neuropathic pain?
A: Carbamazepine, Gabapentin, Pregabalin

Q: What Antiepileptic drug treats trigeminal neuralgia (from Tic Diloreaux)?
A: Carbamazepine

Q: What is the adverse effect of carbamazepine?
A: Steven Johnson Syndrome, Agranulocytosis, but perhaps it’s worth the risk considering trigeminal neuralgia is so painful that people commit suicide.

Q: What Antiepileptic drugs treat post-herpetic neuralgia?
A: Gabapentin, Pregabalin

Q: What local anaesthetic can you use to treat neuropathic pain?
A: Lidocaine

MIGRAINE DRUGS

Q: What drug classes can you use to treat acute migraines?
A: Triptans, Ergots, Anti-emetics, and NSAIDs

Q: Which triptans are long-acting?
A: Frovatriptan, Naratriptan (Frodo is very old hobbit. Narnia is a very old kingdom.)

Q: Which triptans have less side effects than the others?
A: Almotriptan (“good for the alma (spirit)”)

Q: Which triptans do you take intranasally?
A: Sumatriptan, Zolnitriptan (nose is a Summit of your face, and there’s some mountain Gundi knows of that sounds like Zolni)

Q: What are the ergot drugs?
A: Ergotamine Tartrate and Dihydroergotamine Mesylate (DHE)

Q: What are the adverse effects of triptans and ergots?
A: Paresthesia, heaviness in chest

Q: What additional adverse effects do ergots have?
A: muscle cramps, overuse headaches (which defeats the purpose of taking ergots for migraines in the first place)

Q: Which anti-emetic drugs are used to treat migraines?
A: Metoclopramide and Domperidone (which you will probably need after drinking too much Don Perignon)

Q: What are the adverse effects of the anti-emetics?
A: extrapyramidal side effects

Q: What prophylaxis do you use for migraines?
A: beta blockers (propranolol, timolol), antiepileptic drugs.

Q: Which antiepileptic drugs do you use for migraine prophylaxis?
A: Topiramate, Divalproex sodium (“Top Divas” take these to prevent migraines and seizures when they’re singing on stage)

Q: What is the adverse effect of topiramate?
A: Glaucoma

Q: What is the adverse effect of Divalproex sodium?
A: Hepatotoxicity


ADHD DRUGS

Q: What drug classes treat ADHD?
A: “SAGO” —
Stimulants (Methylphenidate, Amphetamines, Mixed Amphetamines (Adderall), Lisdexamfetamine, Pemoline)
Atomoxetine
Guanfacine
Others (Antidepressants (TCA, Bupropion), A2-agonist (clonidine))

Q: Which ADHD drugs are fast-acting?
A: Stimulants

Q: Which ADHD drugs are slow-acting?
A: Atomoxetine, Guanfacine

Q: MOA of stimulants?
A: Release DA

Q: What are the side effects of the stimulants used to treat ADHD?
A: Weight loss, Tourette’s Syndrome, Dependence.

Q: What’s good about Lisdexamfetamine that sets it apart from the other stimulants?
A: It’s the prodrug of d-amphetamine, and therefore you can’t abuse it.

Q: Why isn’t Pemoline used to treat ADHD anymore?
A: Because it causes hepatotoxicity

Q: MOA of Atomoxetine?
A: Norepinephrine reuptake inhibitor (“NE RI”), and therefore increase NE

Q: What are the adverse effects of Atomoxetine?
A: Glaucoma, Suicide

Q: MOA of Guanfacine?
A: alpha-2 agonist, and therefore decrease NE (vs. atomoxetine) and decrease sympathetic tone

Q: What are the adverse effects of Guanfacine?
A: decreased heart rate, decreased sympathetic, somnulence, abdominal pain, hypotension


ALZHEIMER DRUGS

Q: What drugs treat Alzheimer Disease?
A: ACHEIs (acetylcholine esterase inhibitors) and Memantine

Q: What are the ACHEIs?
A: Donepezil, Rivastigmine, Galantamine, Tacrine (Alzheimer patients “Don’t Remember Good Times”) — they increase ACh, giving you more brain stimulation.

Q: What are the adverse effects of ACHEI?
A: diarrhea, weight loss (vs. Memantine, which gives you constipation and dizziness)

Q: MOA for memantine?
A: It is an NMDA antagonist, and therefore decreases Glutamate signal. In Alzheimer’s disease, too much excitation from glutamate causes neurotoxicity, damaging neurons in the brain, which worsens Alzheimers. Memantine is used for severe Alzheimers.

Q: Can you cure Alzheimers with these drugs? What do these drugs really do for Alzheimer patients?
A: No. You can only raise the cognitive performance of patients initially above the baseline. But then after 6 months, it starts declining. Basically with AChEI drugs, you just delay the decline in cognitive performance in the beginning. Once Alzheimers is severe in the patient, then use Memantine.

PARKINSON DRUGS

Q: What kind of drugs can you use to treat Parkinson’s Disease?
A: The inherent problem in Parkinson Disease is the lack of Dopamine. Therefore, you use Dopaminergic drugs, or Anticholinergic drugs. Remember in the Nigro-Striatal-Nigral Feedback loop, ACh stimulates GABA release, which inhibits DA. Therefore if you decrease ACh, you decrease GABA, and increase DA. Also remember that the point is to get DA and ACh levels balanced. So you can do this either by increasing DA or decreasing ACh, and therefore you can use either dopaminergic or anticholinergic drugs.

Q: What dopaminergic drugs can you use for Parkinson treatment?
A: Levodopa + Carbidopa, DA Agonists, COMT Inhibitors, MAO-B Inhibitors, Amantadine (which pretends to be DA).

Q: What anticholinergic drugs can you use to treat Parkinson Disease?
A: M-1 antagonists — Trihexyphenidyl, Benztropine

Q: Why do you give Carbidopa with Levodopa?
A: To prevent Levodopa (which crosses BBB) from converting to Dopamine (which doesn’t cross BBB). Carbidopa inhibits AAD in the periphery of the brain. AAD normally decarboxylates Levodopa into Dopamine. KNOW THIS!!!

Q: What are the adverse effects of Levodopa?
A: Dyskinesia, “Wearing-Off” Effect (loss of efficacy), “On-Off” phenomenon (alternate between benefit and no benefit), Withdrawal –> Neuroleptic Malignant Syndrome

Q: What happens if you give Levodopa with MAOI?
A: Hypertensive crisis… too much DA.

Q: What Dopamine agonists can you use to treat Parkinson Disease?
A: Bromocriptine, Ropinirole, Pramipexole, and Apomorphine (“Bromo goes to PR and gets an A”)

Q: What type of dopamine receptors do the dopamine agonists bind to?
A: Bromocriptine (D2 agonist), Ropinirole and Pramipexole (D2,D3 agonists), Apomorphine (D4 agonist)

Q: Which Dopamine agonist is also an emetic, and can make you throw up?
A: Apomorphine

Q: Which Parkinson drugs can also treat Restless Legs Syndrome?
A: Ropinirole and Pramipexole (D2/D3 agonists)

Q: What’s the adverse effect of Apomorphine?
A: QT Prolongation, Abuse

Q: What drug is best as a “rescue treatment” during the “off” period of Parkinson Disease?
A: Apomorphine

Q: What COMT inhibitors can you use to treat Parkinson?
A: Entacapone (used as adjunct), Tolcapone (gives you hepatotoxicity)

Q: What MAO-B inhibitors can you use?
A: Selegiline (used as adjunct), Rasagiline (gives you hepatotoxicity)

Q: What are the adverse effects of Trihexyphenidyl and Benztropine?
A: Sedation, Confusion

HUNTINGTON DRUGS

Q: What three drug classes can you use to treat Huntingtons?
A: Since the problem is in too much DA due to loss of GABA, you can treat Huntington Disease with D2 antagonists, Monoamine Depleters. You can also treat with cholinergic drugs. The point is to get DA and ACh levels balanced. So this would mean either decreasing DA or increase ACh.

Q: Describe the Nigro-Striatal-Nigral Feedback Loop
A: Substansia Nigra Pars Compacta stimulates Corpus Striatum to produce DA. DA inhibits ACh release. ACh normally stimulates GABA release. GABA inhibits Substantia Nigra from producing DA.

Q: What D2 antagonists can treat Huntington Disease?
A: Risperidone, Haloperidone (which are both also antipsychotics)

Q: What Monoamine depleters can you use to treat Huntington Disease?
A: Tetrabenazine, Reserpine

DRUGS OF ABUSE

Q: Name some stimulants:
A: Cocaine, Amphetamines, Methylphenidate. Remember we can use stimulants for ADHD, but also they can be abused.

Q: Name some depressants:
A: Benzodiazepine, Barbiturates. Remember these can be used for anxiety or epilepsy

Q: Describe EtOH metabolism:
A: EtOH + ADH (alcohol dehydrogenase) –> Acetaldehyde.
Acetaldehyde + ALDH (aldehyde dehydrogenase) –> Acetic Acid
“Wine to vinegar”

Q: How does disulfiram work to treat alcohol abuse?
A: It blocks Aldehyde Dehydrogenase, making you accumulate a lot of aldehyde if you drink alcohol. This makes you feel ill and makes you not want to drink alcohol ever again.

Q: What symptoms do you see in opiate overdose?
A: You depress sympathetic nerves too much — pinpoint pupils, coma, respiratory depression

Q: What symptoms do you see in opiate withdrawal?
A: increased sympathetic — pupil dilation, restlessness

Q: What drug is used to treat heroin withdrawal because it is similar to heroin but has a much longer half life?
A: Methodone. KNOW THIS!!!

Q: What drugs are used to treat opioid toxicity because they are opioid antagonists?
A: Naloxone and Naltrexone

Q: What drug is used to treat both opioid toxicity and alcohol abuse?
A: Naltrexone

Q: What is the maintenance drug for opioid-dependent patients because of its long half-life?
A: Buprenorphine

Q: What drug treats tobacco or smoking addiction?
A: Bupropion, Varenicline (nicotinic partial agonist). KNOW THIS!!!

Q: What kind of agonists are hallucinogens?
A: 5HT agonists

Q: How does Phencyclidine (PCP) work?
A: blocks NMDA, decreasing Glutamate stimulation

Q: What are the signs of phencyclidine intoxication?
A: analgesia, amnesia, stimulant and depressant actions, slurred speech, VERTICAL NYSTAGMUS

Q: What are the signs of phencyclidine overdose?
A: extremely high temperature, rhabdomyolysis, seizures, coma

Q: What substance of abuse is found in antifreeze, windshield washer solution, and paint strippers?
A: Methanol

Q: What happens if you eat windshield wiper fluid?
A: Methanol – blindness

Q: Describe methanol metabolism:
A: Methanol + ADH –> Formaldehyde
Formaldehyde + ALDH –> Formic Acid (which causes metabolic acidosis, lactic acidosis, and OCULAR INJURY/BLINDNESS!!!)

Q: What substance is found in antifreeze, engine coolants, and brake fluids?
A: Ethylene Glycol

Q: What are the three stages of intoxication of ethylene glycol?
A: 1. Neurological stage (metabolic acidosis, CNS depression — 1/2 to 12 hrs) , 2. Cardiopulmonary stage (tachycardia, hypertension — 12-24 hrs), 3. Renal stage (oliguria, tubular necrosis — 24-72 hrs)

Q: Describe Ethylene Glycol metabolism:
A: Ethylene Glycol + ADH –> Glycoaldehyde.
Glycoaldehyde + ALDH –> Glycolate –> Glyoxylate –> Oxalate
KNOW THIS!!!

Q: What is significant about glycolate?
A: it causes the metabolic acidosis in ethylene glycol intoxication

Q: What is significant about oxalate?
A: it crystallizes in the kidneys, causing the renal damage seen in ethylene glycol intoxication

Q: How do you treat the metabolic acidosis found in methanol and ethylene glycol?
A: treat wit sodium bicarbonate

Q: How do you treat methanol and ethylene glycol overdose?
A: You give the patient EtOH. The EtOH competes with the methanol and ethylene glycol in binding alcohol dehydrogenase, preventing the methanol and ethylene glycol from getting metabolized into the harmful products.

Q: How do you increase the elimination of methanol and ethylene glycol during overdose?
A: Give patient folic acid or hemodialysis if its really bad.



SCHIZOPHRENIA DRUGS (ANTIPSYCHOTIC DRUGS)

Q: What is the key to treating Schizophrenia?
A: antagonizing D2, and if you’re really good, antagonizing D2 and 5HT-2

Q: Why D2 and 5HT2?
A: Because D2 works in the brain and 5HT-2 is responsible for increasing CNS and cardiovascular stimulation.

Q: In what four pathways do you find D2 receptors?
A: 1. Mesolimbic pathway — a decrease in D2 causes antipsychotic effects. This is what we target in Schizophrenia.

2. Mesocortical pathway — a decrease in D2 causes antipsychotic effects. This is what we target in Schizophrenia.
3. Nigrostriatal pathway — a decrease in D2 causes parkinsonism or Extrapyramidal Symptoms (EPS).
4. Tuberoinfundibular pathway — a decrease in D2 causes increase in prolactin.

Q: What is the difference between the positive and negative symptoms of schizophrenia?
A: positive: delusions, hallucinations
negative: apathy, anhedonia, flat affect

Q: Which generation antipsychotic drugs treats both positive and negative symptoms?
A: second generation. first generation only treats positive symptoms of schizophrenia.

Q: Which generation antipsychotic drugs block D2 only?
A: First generation blocks D2 only, whereas second generation blocks both D2 and 5HT-2 (except aripiprazole, which antagonizes 5HT-2 but is partial agonist to D2)

Q: What are the three types of phenothiazines (which is a first generation antipsychotic)?
A: Aliphatic, Piperidine, Piperazine (which remember is an antihistamine)

Q: Which phenothiazine causes the most orthostatic hypotension?
A: Aliphatic

Q: Which phenothiazine causes more sedation?
A: Piperidine

Q: Which phenothiazine causes more EPS?
A: Piperazine

Q: Which Piperidine causes retinal pigmentation if given over 800 mg/day?
A: Thioridazine. KNOW THIS!!!

Q: Which first generation antipsychotic drug is the most potent, and only adverse effect is EPS?
A:Haloperidol (which is a butyrophenone)

Q: What are the major side effect of conventional (first-generation) antipsychotics?
A: Extrapyramidal symptoms (EPS), Neuroleptic Malignant Syndrome. Not as much in second generation.

Q: What is it called when a patient on antipsychotics suddenly have muscle rigidity, autonomic instability, elevated CPK, and changing levels of consciousnes?
A: Neuroleptic Malignant Syndrome. It is an emergency and can lead to death.

Q: Why do antipsychotics also often cause orthostatic hypotension and sedation?
A: Because they also block H1, M1, and A1 — Multiple Receptor Effects.

Q: What stage of extrapyramidal symptoms (EPS) do you find acute dystonic reaction (torticolis) and parkinsonian syndrome?
A: Early stage. KNOW THIS!!!

Q: Remember what you use to treat torticolis from Pharm I?
A: Botulinum toxin

Q: What stage of EPS do you find Akathisia, which is when the patient moves around a lot as if they can’t sit down?
A: Intermediate stage.

Q: What do you find at the late stage of EPS?
A: Tardive Dyskinesia — when the patient involuntarily moves the mouth a lot.

Q: What is the major adverse effect of Clozapine (second generation)?
A: Agranulocytosis (like carbamazepine), and seizures

Q: Which antipsychotic drug has very little EPS because only 40-50% of it work on Nigrostriatal pathway, which is what causes the EPS/Parkinsonian symptoms?
A: Clozapine (second generation)

Q: What is the major adverse effect of olanzapine (second generation)?
A: Significant weight gain

Q: What is the major adverse effect of quetiapine (second generation)?
A: Cataracts (“Catiapine”)

Q: Which second generation antipsychotic can give you nasal congestion?
A: Iloperidone (think of Ilu with a stuffy nose)

Q: Which second generation antipsychotic treats patients with Schizophrenia and Depression/Anxiety?
A: Ziprasidone

Q: Which second generation antipsychotics particularly give you QT prolongation?
A: Ziprasidone and Iloperidone

Q: Which second generation antipsychotic treats Schizophrenia, Bipolar disorder, and Restless Leg Syndrome?
A: Asenapine

Q: Which second generation antipsychotics cause the most weight gain?
A: From most to least weight gain: Clozapine –> Olanzapine –> Risperidone — “COR”

Q: Which second generation antipsychotic drug is unique in that it is a 5HT-2 antagonist but a D2/5HT1 partial agonist?
A: Aripiprazole

Block 2 Prep Questions

Q: Which drugs give you heterochromia iridis?
A: Prostaglandin Analogues (Latanoprost, Bimatoprost, Travoprost)

Q: Which drug is used to treat a patient with both Schizophrenia and Bipolar?
A: Asenapine (D2, 5HT-2 Antagonist)

Q: Which drug gives you nasal congestion?
A: Iloperidone (Second generation schizophrenia drug, D2/5HT2 Antagonist)

Q: Which class of drugs give you hoarseness and thrush?
A: Steroids (i.e. those used in asthma. They give you thrush because they immunosuppress)

Q: Which drug do you use to treat seasonal allergies?
A: Fluticasone propionate (asthma steroid)

Q: Which drug gives you QT prolongation?
A: Ziprasodone, Iloperidone (second generation schizophrenia drug), Apomorphine (emetic, parkinson)

Q: What does ipratropium treat? What’s the adverse effect? Mode of action?
A: Asthma, COPD. AE: dry mouth. MOA: muscarinic blocker.

Q: Which second generation schizophrenia drug do you have little EPS?
A: Clozapine, because only 40-50% drug work on nigrostriatal D2 pathway.

Q: What drugs do leukotriene modifiers increase?
A: warfarin, theophylline, and terfenadine.

Q: What’s the difference between terfenadine and terbutaline?
A: Terfenadine – Second gen antihistamine Rx Allergies.
Terbutaline
– B2 agonist Rx Asthma.

Q: What’s the difference between bupropion and buspirone?
A: Bupropion – NE/DA Reuptake inhibitor. Rx Smoking, Depression.
Buspirone
– 5HT-1A partial agonist post-synaptically and full agonist pre-synaptically (autoreceptor). Rx Anxiety.

Q: What’s the difference between Cimetidine and Cetirizine?
A: Cimetidine – Rx Peptic Ulcers. Gives you gynecomastia because binds testosterone receptor.
Cetirizine – Rx Allergies. Second gen antihistamine (H1 specific). Kids metabolize it faster.

Q: What is “History on TLC”?
A: Terfenadine, Loratadine, Cetirizine – Second generation antihistamines.

Q: What do you treat with Cisapride?
A: 5HT4 agonist –> increase GI motility –> Rx GERD. AE: Fatal arrythmias.

Q: What anti-emetic drug is a muscarinic antagonist?
A: Hyoscine

Q: Which anti-emetic drugs work only in vestibular nucleus and not CTZ (and therefore only treat Motion Sickness)?
A: Cinnarizine, Cyclizine, Promethazine, Hyoscine.

Q: What are Endothelin-1 blockers used for?
A: Rx Pulmonary Hypertension.

Q: Which endothelin-1 blocker blocks both alpha and beta endothelin?
A: Bosentan.

Q: What drug do you use if you use too much phenylephrine?
A: Thymoxamine, Dapiprazole – Alpha-1 antagonists – reverses pupil dilation from phenylephrine, a glaucoma drug.

Q: What is the best class of drugs for glaucoma?
A: Carbonic Anhydrase Inhibitors – Acetazolamide, Methazolamide, Dichlorphenamide, Dorzalamide, Brinzolamide. They all have zol or zal except dichlorphenamide.

Q: Which drugs dehydrates vitreous body?
A: Glycerine (100% IV), Mannitol (20% IV)

Q: When is carbonic anhydrase inhibitors contraindicated for glaucoma?
A: Sulpha allergies (i.e. allergic to penicillin), Digoxin use, pregnancy.

Q: Which glaucoma drug is an alpha-1 agonist?
A: Phenylephrine – constricts vessels –> decrease aqueous humor production –> Rx congestion.

Q: Which glaucoma drugs are alpha-2 agonists?
A: Brimonidine, apraclonidine (negative feedback –> decrease aqueous humor production, increase outflow)

Q: Which drug is used to treat both glaucoma and eyelash lice?
A: Physostigmine – anticholinesterase – increase ACh – constrict pupillary sphincter –> increase outflow through trabecular meshwork.

Q: Which drug is an irreversible cholinergic agonist for Rx of Glaucoma?
A: Phosphate Iodide. AE – Apnea (can’t dilate bronchioles)

Q: What drugs do you use for fundoscopy and glaucoma?
A: You want’ to dilate the eyes, so you use cholinergic antagonists – paralyze sphincter muscles: Tropicamide (shortest acting).

Q: Which heavy metal gives you erethism (red palms)?
A: Elemental Mercury.

Q: Which fecal-bulking drug do you not give to patients with renal stones?
A: Calcium Polycarbophil – because it has calcium.

Q: Which heavy metal interferes with Vitamine D Synthesis in renal tubular cells?
A: Lead –> brittle bones, growth arrest in kids.

Q: Which local anaesthesia gives you methemoglobin as an adverse effect?
A: Prilocaine.

Q: Local anaesthetics are metabolized by what?
A: Ester are metabolized by plasma cholinesterase.
Amides are metabolized by CYP450.

Q: All local anaesthetics are vasodilators except…?
A: Cocaine – vasoconstrictor. Because most are vasodilators, the duration of action is short, so you co-give it with a constrictor, like epinephrine.

Q: What drug do you use to treat Schizoaffective disorder?
A: Paliperidone – the active metabolite of Risperidone, a second generation schizophrenia drug.

Q: Which drugs give you diplopia?
A: Carbamazepine, Phenytoin, Lamotrigine, and Gabapentin

Q: Which drugs do you use to treat Lennox-Gastaut Syndrome?
A: Lamotrigine, Felbamate, and Topiramate

Q: Which drugs give you aplastic anemia?
A: Ethosuxamide, Felbamate.

Q: What drug treats status epilepticus?
A: Benzodiazepine.

Q: What drug gives you glaucoma?
A: Atomoxetine (Rx ADHD), Topiramate (Rx Epilepsy)

Q: What drug gives you retinal pigmentation?
A: Thioridazine, which is a piperidine, which is a phenothiazine, which is a first generation schizophrenia drug).

Q: What’s the most potent first generation schizophrenia drug?
A: Haloperidol.

Q: Which drugs do you use to treat post-herpetic neuralgia?
A: Pregabalin and Gabapentin

Q: Which drugs do you use to treat trigeminal neuralgia (Tic Delaroux)
A: Carbamazepine

Q: Which drugs do you use to treat ADHD?
A: SAGO – Stimulants, Atomoxetine, Guanfacine, Others (Bupropion, TCA, clonidine)

Q: What is a sign of opiate overdose? opiate withdrawal?
A: Overdose – respiratory depression, pinpoint pupils.
Withdrawal – restlessness, dilated pupils.

Q: What is the maintenance drug to treat opioid-dependent patients?
A: Buprenorphine – because it has a long half-life.

Q: Which drugs block NMDA (decrease glutamate)?
A: Memantine (Alzheimer drug), Phencyclidine (illicit drug)

Q: Which COMT inhibitor gives you hepatotoxicity?
A: Tolcapone (Rx Parkinson).

Q: Which MAO-B inhibitor gives you hepatotoxicity?
A: Rasagiline (Rx Parkinson).

Q: What do you use to treat steroid dependence?
A: Troleandomycin, Cyclosporin, Gold, Methotrexate.

Q: Which schizophrenia drug gives you cataracts?
A: Quetiapine – second generation schizophrenia drug.

Q: Which anti-diarrheal drug is an opioid agonist?
A: Loperamide – binds mu receptors –> decrease GI motility.

Q: Which serotonin antagonist is used to treat hypertension?
A: Ketanserin – 5HT2 and alpha antagonist.

Q: Which serotonin antagonist is used to treat nausea and vomiting during chemotherapy?
A: Ondansetron – 5HT3 antagonist.

Q: Which antihistamine do you give just once a day?
A: Loratadine.

Q: Which endothelin-1 blocker is a non-sulfonamide?
A: Ambrisentan. Prescribe this if patient is allergic to sulfonamides.

Q: Which drug is a PGE2 analogue?
A: Dinoprostone – relaxes smooth muscle –> induce labor, abortion.

Q: What can you treat with Methysergide and Cyproheptadine?
A: Serotonin Syndrome (Hypertensive crisis), Carcinoid tumor, migraines. They are 5HT-2 antagonists.

Q: Which antacid gives you diarrhea?
A: Magnesium Hydroxide.

Q: What do you use to treat Zollinger-Ellison Syndrome?
A: Too much gastrin. Rx with H2 receptor antagonists (Cimetidine, Ranitidine, Nizatidine, Famotidine) or Proton Pump inhibitor (Omeprazole).

Q: Which H2 receptor antagonist gives you gynecomastia?
A: Cimetidine.

Q: What does lactulose treat?
A: Constipation, Hepatic encephalopathy. It is an osmotic agent.

Q: Which IBD drug is not only an anti-inflammatory but also an anti-bacterial?
A: Sulfasalazine

Q: Which IBD drugs are coated (so they don’t release until get to colon)?
A: Mesalamine, Budesonide – slow acting.

Q: Which IBD drug is an antispasmodic?
A: Dicyclomine

Q: Which type of serotonin receptors do ergot alkaloids block?
A: 5HT-1 and 2

Q: Which cholinergic antagonists are used to treat peptic ulcers?
A: Propantheline, Isopropamide, Scopolamine. “To be anti-colin, scolding is proper.”

Q: Sulcralfate requires what?
A: H+, to crosslink into polymer –> bind to exposed protein in ulcer.

Q: What is the most potent corticosteroid in the treatment of glaucoma?
A: Fluorometholone – potency of 40-50. Vs. hydrocortisone (potency 1)

Q: Which heavy metal gives you thirst, garlic taste?
A: Arsenic

Q: Which drugs gives you Stevens-Johnson Syndrome?
A: Carbamazepine, Ethosuxamide, Lamotrigine (“Steve likes carbs and succulent lambs”)

Q: What happens if you eat antifreeze?
A: Ethylene glycol – renal failure

Q: What happens if you eat windshield wiper fluid?
A: Methanol – blindness

Q: Which substances give you metabolic acidosis?
A: methanol, Ethylene glycol.

Q: How do you treat methanol and ethylene glycol poisoning?
A: Rx metabolic acidosis with NaHCO3 (base).
Inhibit metabolism with EtOH
Increase elimination with Folic Acid.

Q: What beta-2 agonist is used as a preventative drug for asthma?
A: Salmeterol – long lasting.

Q: What is the primary adverse effect of SSRI?
A: Sexual dysfunction.

Q: Which second generation schizophrenic drug gives you the most weight gain?
A: Clozapine. Olanzapine gives you a lot too.

Q: Which drugs treat Restless Legs Syndrome?
A: Asenapine (second gen schizophrenic drug),Ropinirole, Pramipexole (DA agonists used in Parkinson).

Q: Which Parkinson drug is used as a “rescue treatment” during the “off” periods of levadopa?
A: Apomorphine.

Q: What form of Iron is 90% absorbed?
A: Ferrous (Fe++) iron.

Q: What are you testing with the Schilling Test?
A: Pernicious Anemia (8-35% radioactive B12 in urine means normal)

Q: How many days does it take fiber to be effective?
A: 2-4 days.

Q: Which drug gives you oral hypoesthesia?
A: Asenapine

Q: Which drugs are P450 Inhibitors?
A: PICK EGS – Protease inhibitors, Isoniazid, Cimetidine, Ketonazoles (all azoles), Erythromycin, Grapefruit Juice, Sulfonamides

Q: Which drugs induce P450?
A: “Car Bar et Phen Fam” – Carbamazepine, Barbiturates, EtOH, Phenytoin, Rifampin.

Q: What’s the half-life of Cadmium?
A: 30 years

Q: What do you get with cadmium toxicity?
A: Bronchospasm and Hemoptysis –> Tubular and globerular damage –> Osteomalacia and Osteoporosis.

Q: What does Cadmium do that is toxic?
A: It displaces metals from metalloenzymes.

Q: What is the adverse effect of B12 treatment for Pernicious Anemia?
A: Hypokalemia. Eat bananas!

Q: What IBD treatment is a TNF-alpha inhibitor?
A: Infliximab

Q: What is the drug of choice for IBD?
A: Sulfasalazine

Q: What do you use to treat Crohn’s Disease with fistula?
A: Cyclosporine, an immunosuppressant.

Q: How do you calculate how much iron you need?
A: Iron needed (g) = (15 – Hb/g%) x body weight (kg) x 3

Q: What do you use for GERD treatment?
A: Antiemetics that are also promotility agents — Domperidone and Metoclopramide, which both antagonize DA.

Q: What are the monoamine depleters?
A: Tetrabenazine and Reserpine — used in Huntington Disease.

Q: What do you give with Levodopa?
A: Carbidopa, which blocks AAD and prevents Levodopa (lipid-soluble) from becoming Dopamine before reach brain.

Q: What do you use amantadine for?
A: Parkinson Disease — pretends to be DA.

Q: What are the AChEIs?
A: “Don’t Remember Good Times” – Donepezil, Rivastigmine, Galantamine, Tacrine (which isn’t used much anymore) — treats Alzheimer Disease.

Q: What M-1 antagonists do you use to treat Parkinsons?
A: Trihexyphenidyl and Benztropine. Decrease ACh –> Decrease GABA –> Increase DA.