CNS Pharmacology (SUDWEEKS) Flashcards
Which of the following are “Typical antipsychotics”?
A. Clozapine
B. Olanzapine
C. Phenothiazines
D. Risperidone
C. Phenothiazines
Discuss the Dopamine hypothesis:
Hyperactive dopamine pathway causes psychosis.
There are “typical antipsychotics” and “atypical antipsychotics” that both are dopamine antagonist
Which of the following are “Typical antipsychotics”?
A. Clozapine
B. Olanzapine
C. Chlorpromazine
D. Risperidone
C. Chlorpromazine
note: chlorpromazine is a derivative of phenothiazine
Which of the following is the most widely prescribed “Typical antipsychotics”?
A. Clozapine
B. Olanzapine
C. Haloperidol
D. Risperidone
C. Haloperidol
______ is the most widely prescribed “typical antipsychotic”.
Haloperidol
“Typical” antipsychotics can cause all of the following EXCEPT:
A. Tardive dyskinesias
B. Parkinson like symptoms
C. Dystonias (spasms)
D. Perioral tremor
E. “Typical” antipsychotics can cause all of the above
E. “Typical” antipsychotics can cause all of the above
note: “typical” antipsychotics can cause perioral tremor - “Rabbit syndrome”
Clozapine is an _______.
A. “typical” antipsychotic
B. “atypical” antipsychotic
B. “atypical” antipsychotic
Discuss “Typical” vs “Atypical” antipsychotics:
Both of them block D2 receptors (dopamine)
“Typical” Antipsychotics:
- 1st generation dopamine antagonist
- Eg. Chlorpromazine and Haloperidol
- Can cause:
- Tardive dyskinesias
- Parkinson like symptoms
- Dystonias (spasms)
- Perioral tremor “Rabbit syndrome”
“Atypical” Antipsychotics:
- Newer (2nd generation” D2 antagonist
- Less likely to develop tardive dyskinesias
- Eg. Clozapine
- some also block 5HT-2 receptors
How can you manage the extrapyramidal motor effects of antipsychotics?
By using Antimuscarinic drugs
- ACh and dopamine oppose each other in the basal ganglia, so blocking muscarinic receptors tends to balance out the blocking of the dopamine receptors by the antipsychotic drugs
Discuss Neuroleptic Malignant Syndrome:
Neuroleptic Malignant Syndrome
- A life-threatening neurological disorder that is an adverse rxn to antipsychotic drugs
What is the desired mechanism of action of antipsychotics?
Dopamine blockers
What are other adverse effects of antipsychotic use?
- Antimuscarinic symptoms (from the antimuscarinic drugs used to tx antipsychotic drug side effects): constipation, dry mouth, bradycardia
- Orthostatic hypotension
- Convulsions
- Photosensitivity
- Cardiac arrhythmias (long QT syndrome)
- Galactorrhea (Dopamine is “PIH” Prolactin Inhibiting Hormone
What are the common side effects of antipsychotic drugs?
Extrapyramidal motor effecs
- Tardive dyskinesias (jerky movements)
- Parkinson like symptoms
- Dystonias (spasma)
- Perioral tremor “Rabbit Syndrome”
_______ are the 3rd most common prescription drugs taken by americans of all ages.
Antidepressants
Discuss the difference between Unipolar vs Bipolar depression:
Unipolar: mood changes in one direction
- stress related, not genetic
Bipolar: less common than unipolar
- hereditary
- oscillates between manic and depressive
Which of the following is a selective serotonin reuptake inhibitor (SSRI)?
A. Amitriptyline
B. Fluoxetine
C. Venlafaxine
D. Duloxetine
E. Bupropion
B. Fluoxetine
Amitriptyline = Tricyclic antidepressant (TCAs)
Fluoxetine = Selective Serotonin Reuptake Inhibitor (SSRIs)
Venlafaxine = mixed 5-HT and NE Reuptake Inhibitors (SNRIs)
Duloxetine = mixed 5-HT and NE Reuptake Inhibitors (SNRIs)
Bupropion = Norepinephrine Reuptake inhibitor
Which of the following is a Norepinephrine reuptake inhibitor?
A. Amitriptyline
B. Fluoxetine
C. Venlafaxine
D. Duloxetine
E. Bupropion
E. Bupropion (Wellbutrin)
Amitriptyline = Tricyclic antidepressant (TCAs)
Fluoxetine = Selective Serotonin Reuptake Inhibitor (SSRIs)
Venlafaxine = mixed 5-HT and NE Reuptake Inhibitors (SNRIs)
Duloxetine = mixed 5-HT and NE Reuptake Inhibitors (SNRIs)
Bupropion = Norepinephrine Reuptake inhibitor
Which of the following is Tricyclic antidepressant (TCAs)?
A. Amitriptyline
B. Fluoxetine
C. Venlafaxine
D. Duloxetine
E. Bupropion
A. Amitriptyline
note: it has “tri” in the name
Amitriptyline = Tricyclic antidepressant (TCAs)
Fluoxetine = Selective Serotonin Reuptake Inhibitor (SSRIs)
Venlafaxine = mixed 5-HT and NE Reuptake Inhibitors (SNRIs)
Duloxetine = mixed 5-HT and NE Reuptake Inhibitors (SNRIs)
Bupropion = Norepinephrine Reuptake inhibitor
Which of the following is a mixed 5-HT and NE reuptake inhibitor (SNRIs)?
A. Amitriptyline
B. Fluoxetine
C. Venlafaxine
D. Duloxetine
E. Bupropion
C. Venlafaxine
D. Duloxetine
Amitriptyline = Tricyclic antidepressant (TCAs)
Fluoxetine = Selective Serotonin Reuptake Inhibitor (SSRIs)
Venlafaxine = mixed 5-HT and NE Reuptake Inhibitors (SNRIs)
Duloxetine = mixed 5-HT and NE Reuptake Inhibitors (SNRIs)
Bupropion = Norepinephrine Reuptake inhibitor
Which of the following is a Monoamine Oxidase Inhibitor (MAOIs)?
A. Amitriptyline
B. Fluoxetine
C. Phenelzine
D. Duloxetine
E. Bupropion
C. Phenelzine
note: these should not be used together w/ other antidepressant drugs, or w/ autonomic drugs that cause the release of catecholamines or serotonin
All of the following are side effects of SSRIs EXCEPT:
A. Nausea
B. Anorexia
C Insomnia
D. Dry mouth
E. Loss of libido
D. Dry mouth
SSRI side effects:
- Nausea
- Anorexia
- Insomnia
- Loss of libido
TCAs side effects:
- Initial use:
- sedation
- confusion
- motor impairment
- Other effects:
- dry mouth
- blurred vision
- urinary retention
- postural hypotension
- Ventricular dysrhythmias
List the side effects of TCAs:
TCAs side effects
Initial use:
- sedation
- confusion
- motor impairment
- (these side effects usually wear off in days)
Other effects:
- dry mouth
- blurred vision
- urinary retention
- postural hypotension
- continued sedation in some, overdose –> ventricular dysrhythmias
List the side effects for Monoamine receptor antagonist and MAOIs:
Monoamine receptor antagonist
- constipation
- increased appetite
- weight gain
- somnolence
MAOIs
- hypotension
- tremors
- exitement
- insomnia
- increased appetite
- weight gain
- dry mouth
- bluurred vision
- urinary retention
- Interacts with foods containing tyramine (i.e. cheese and fermented compounds
- Drug interactions can be life-threatening
Which of the following drugs counteract with tyramine containing foods (i.e. cheese and fermented compounds)?
A. SSRIs
B. Monoamine receptor antagonist
C. TCAs
D. MAOIs
D. MAOIs
Which of the following is the most commonly prescribed antidepressants?
A. SSRIs
B. Monoamine receptor antagonist
C. TCAs
D. MAOIs
A. SSRIs
note: generally have the fewest severe side effects, and high therapeutic index
List other clinical uses for each of the following:
- TCAs
- TCAs and SSRIs
- SSRIs
- Buproprion
- TCAs for neuropathic pain
- TCAs and SSRIs for fibromyalgia
- SSRIs for anxiety disorders
- SSRIs for ADHD
- Buproprion (NE uptake blocker) for addiction
Which of the following is a Monoamine receptor antagonist (i.e. alpha2 blocker)?
A. Trazodone
B. Mirtazapine
C. St. John’s wort
D. Esketamine
B. Mirtazapine
Trazodone: thought to potentiate 5HT activity (get mixed agonist, antagonist activity) and blocks alpha1 receptors
Mirtazapine: monoamine receptor antagonist (alpha2 blocker)
St. John’s wort: (contain hyperforin) a weak monoamine uptake inhibitor that activates P450 enzymes
Esketamine: S-enantiomer of ketamine (general anesthetic) that blocks NMDA receptors
Which of the following is a weak monoamine uptake inhibitor that activates P450 enzymes?
A. Trazodone
B. Mirtazapine
C. St. John’s wort
D. Esketamine
C. St. John’s wort
Trazodone: thought to potentiate 5HT activity (get mixed agonist, antagonist activity) and blocks alpha1 receptors
Mirtazapine: monoamine receptor antagonist (alpha2 blocker)
St. John’s wort: (contain hyperforin) a weak monoamine uptake inhibitor that activates P450 enzymes
Esketamine: S-enantiomer of ketamine (general anesthetic) that blocks NMDA receptors
Which of the following is thought to potentiate 5HT activity (get mixed agonist, antagonist activity) and also blocks alpha1 receptors?
A. Trazodone
B. Mirtazapine
C. St. John’s wort
D. Esketamine
A. Trazodone
Trazodone: thought to potentiate 5HT activity (get mixed agonist, antagonist activity) and blocks alpha1 receptors
Mirtazapine: monoamine receptor antagonist (alpha2 blocker)
St. John’s wort: (contain hyperforin) a weak monoamine uptake inhibitor that activates P450 enzymes
Esketamine: S-enantiomer of ketamine (general anesthetic) that blocks NMDA receptors
Which of the following is an S-enantiomer of ketamine (general anesthetic) given as a nasal spray that blocks NMDA receptors?
A. Trazodone
B. Mirtazapine
C. St. John’s wort
D. Esketamine
D. Esketamine
Trazodone: thought to potentiate 5HT activity (get mixed agonist, antagonist activity) and blocks alpha1 receptors
Mirtazapine: monoamine receptor antagonist (alpha2 blocker)
St. John’s wort: (contain hyperforin) a weak monoamine uptake inhibitor that activates P450 enzymes
Esketamine: S-enantiomer of ketamine (general anesthetic) that blocks NMDA receptors
Which of the following is a newly approved antidepressant?
A. Trazodone
B. Mirtazapine
C. St. John’s wort
D. Esketamine
D. Esketamine
Which of the following blocks NMDA receptors?
A. Trazodone
B. Mirtazapine
C. St. John’s wort
D. Esketamine
D. Esketamine
Which of the following is an S-enantiomer of ketamine (general anesthetic)?
A. Trazodone
B. Mirtazapine
C. St. John’s wort
D. Esketamine
D. Esketamine
note: esketamine is given as a nasal spray
Which of the following has to be taken under doctor’s supervision and is contraindicated in pts w/ hypertension?
A. Trazodone
B. Mirtazapine
C. St. John’s wort
D. Esketamine
D. Esketamine
Which of the following contains hyperforin?
A. Trazodone
B. Mirtazapine
C. St. John’s wort
D. Esketamine
C. St. John’s wort
Which of the following get mixed agonist/antagonist activity?
A. Trazodone
B. Mirtazapine
C. St. John’s wort
D. Esketamine
A. Trazodone
List 3 drugs used to tx bipolar depression:
Lithium, Valproate and Olanzapine
Which of the following is an atypical antipsychotic?
A. Lithium
B. Valproate
C. Olanzapine
D. Diazepam
C. Olanzapine
Which of the following is a mixed dopamine and 5HT2 receptor antagonist?
A. Lithium
B. Valproate
C. Olanzapine
D. Diazepam
C. Olanzapine
_______ is a prolactin inhibiting hormone that may lead to galactorrhea.
Dopamine
Which of the following is an antiepileptic drug?
A. Lithium
B. Valproate
C. Olanzapine
D. Diazepam
B. Valproate
Which of the following is an anti-mania or “Mood stabilizing drug”?
A. Lithium
B. Valproate
C. Olanzapine
D. Diazepam
A. Lithium
Which of the following is used prophylactically to avoid manic-depressive episodes?
A. Lithium
B. Valproate
C. Olanzapine
D. Diazepam
A. Lithium
Lithium toxicity: nausea, diarrhea, convulsions, coma, hyperreflexia, cardiac arrhythmias, hypotension, thyroid effects, polyuria
- Dietary Na+ restriction leads to increaed lithium retention in the kidneys and can lead to toxicity
Which of the following has a narrow therapeutic index?
A. Lithium
B. Valproate
C. Olanzapine
D. Diazepam
A. Lithium
note: careful with lithium toxicity
Most ______ work by activating or enhancing chloride channels (GABA-A receptors).
Sedative hypnotics
GABA-A receptors also have allosteric binding sites
- BZ1 site (omega-1)
- BZ2 site (omega-2)
List some uses for sedative hypnotics:
- antianxiety
- panic disorders
- sedation
- anticonvulsants
- amnesia
- insomnia
- skeletal muscle relaxation (particularly baclofen)
List some adverse effects of Sedative Hypnotics:
Adverse effects
- ataxia
- confusion
- excessive sedation
- amnesia
- altered sleep patterns
_______ and _______ enhance effect of native GABA on GABA-A receptors (modulators, not direct agonist).
Benzodiazepines and Barbiturates
note: barbiturates at higher doses also inhibit AMPA (glutamate) receptors
All of the following are classified as Barbiturates EXCEPT:
A. Phenobarbital
B. Diazepam
C. Thiopental
D. Pentobarbital
B. Diazepam
Barbiturates = Phenobarbital, Pentobarbital, Thiopental
Benzodiazepines = Diazepam
Which of the following is a Benzodiazepine?
A. Phenobarbital
B. Diazepam
C. Thiopental
D. Pentobarbital
B. Diazepam
Which of the following is a long acting Barbiturate used to tx epilepsy?
A. Phenobarbital
B. Diazepam
C. Thiopental
D. Pentobarbital
A. Phenobarbital
Long acting =Phenobarbital
Intermediate acting = Pentobarbital
Short acting = Thiopental
Which of the following is a intermediate acting Barbiturate sometimes used for sleep induction?
A. Phenobarbital
B. Diazepam
C. Thiopental
D. Pentobarbital
D. Pentobarbital
Long acting =Phenobarbital
Intermediate acting = Pentobarbital
Short acting = Thiopental
Which of the following is a short acting Barbiturate used as an induction anesthetic?
A. Phenobarbital
B. Diazepam
C. Thiopental
D. Pentobarbital
C. Thiopental
Long acting =Phenobarbital
Intermediate acting = Pentobarbital
Short acting = Thiopental
Which of the following is used to tx epilepsy?
A. Phenobarbital
B. Diazepam
C. Thiopental
D. Pentobarbital
A. Phenobarbital
Which of the following is used for sleep induction?
A. Phenobarbital
B. Diazepam
C. Thiopental
D. Pentobarbital
D. Pentobarbital
Which of the following is an induction anesthetic?
A. Phenobarbital
B. Diazepam
C. Thiopental
D. Pentobarbital
C. Thiopental
Which of the following is contraindicated in certain types of porphyria (genetic condition affecting heme synthesis)?
A. MAOIs
B. SSRIs
C. Benzodiazepines
D. Barbiturates
D. Barbiturates
Which of the following have active metabolites that extends the functional half-life?
A. Metoprolol
B. Clonidine
C. Diazepam
D. Phenobarbital
E. Pentobarbital
C. Diazepam
Which of the following act on GABA-A receptors (BZ1 receptor site) and has a low risk of dependence?
A. Buspirone
B. Baclofen
C. Chloral Hydrate
D. Zolpidem
E. Flumazenil
D. Zolpidem
- Not anticonvulsant
- used mainly to tx insomnia
Buspirone = partial agonist at 5-HT1A receptors
Baclofen = GABA-B agonist
Chloral Hydrate = used in dentistry for conscious sedation
Zolpidem = GABA-A agonist (BZ1 recceptor site)
Flumazenil = GABA-A antagonist
Which of the following has a similar action as bezodiazepines but is used as a short acting sleep inducer?
A. Buspirone
B. Baclofen
C. Chloral Hydrate
D. Zolpidem
E. Flumazenil
C. Chloral Hydrate
- used for conscious sedation in dentistry, repetitive doses should not be used
- can result in serious cardiac toxicities if not controlled
Buspirone = partial agonist at 5-HT1A receptors
Baclofen = GABA-B agonist
Chloral Hydrate = used in dentistry for conscious sedation
Zolpidem = GABA-A agonist (BZ1 recceptor site)
Flumazenil = GABA-A antagonist
Which of the following is a GABA-A antagonist that will reverse sedation from drugs acting at BZ sites?
A. Buspirone
B. Baclofen
C. Chloral Hydrate
D. Zolpidem
E. Flumazenil
E. Flumazenil
Buspirone = partial agonist at 5-HT1A receptors
Baclofen = GABA-B agonist
Chloral Hydrate = used in dentistry for conscious sedation
Zolpidem = GABA-A agonist (BZ1 recceptor site)
Flumazenil = GABA-A antagonist
Which of the following is a GABA-B agonist?
A. Buspirone
B. Baclofen
C. Chloral Hydrate
D. Zolpidem
E. Flumazenil
B. Baclofen
- G-protein linked receptor, not an ion channel, activates Gi, leads to decreased cell activity. Sometimes used to treat trigeminal neuralgia
Buspirone = partial agonist at 5-HT1A receptors
Baclofen = GABA-B agonist
Chloral Hydrate = used in dentistry for conscious sedation
Zolpidem = GABA-A agonist (BZ1 recceptor site)
Flumazenil = GABA-A antagonist
Which of the following block H1 receptors in CNS to cause sedation?
A. Buspirone
B. Baclofen
C. Diphenhydramine
D. Zolpidem
E. Flumazenil
C. Diphenhydramine
Buspirone = partial agonist at 5-HT1A receptors
Baclofen = GABA-B agonist
Zolpidem = GABA-A agonist (BZ1 recceptor site)
Flumazenil = GABA-A antagonist
Diphenhydramine = H1 receptor blocker
Which of the following is a partial agonist at 5-HT1A receptors (NOT GABA)?
A. Buspirone
B. Baclofen
C. Diphenhydramine
D. Zolpidem
E. Flumazenil
A. Buspirone
Buspirone = partial agonist at 5-HT1A receptors
Baclofen = GABA-B agonist
Zolpidem = GABA-A agonist (BZ1 recceptor site)
Flumazenil = GABA-A antagonist
Diphenhydramine = H1 receptor blocker
Which of the following is not clinically used bc it likely affects multiple targets including GABA-A?
A. Buspirone
B. Baclofen
C. Diphenhydramine
D. Zolpidem
E. Ethanol
E. Ethanol
Buspirone = partial agonist at 5-HT1A receptors
Baclofen = GABA-B agonist
Zolpidem = GABA-A agonist (BZ1 recceptor site)
Flumazenil = GABA-A antagonist
Diphenhydramine = H1 receptor blocker
Ethanol = affects multiple targets not clinically used
Which of the following is a sedative hypnotic?
A. Methocarbamol
B. Carisoprodol
C. Cyclobenzaprine
D. Two of the above
E. All of the above
E. All of the above
note: all of these answer choices are sedative hypnotics that have less described mechanisms of action
Discuss Epilepsy:
Epilepsy
- Seizures - inappropriate and excessive activity of CNS neurons
- Partial seizures are limited to one side of the brain at onset
- 2 types of generalized seizures:
- Tonic-clonic (grand mal)
- Absence (petit mal)
Discuss the mechanisms of action for Antiepileptics?
Antiepileptics
- NaV+ channels antagonist
- Ca2+ channel antagonist
- Glutatmate receptor antagonist (AMPA, NMDA)
- Cl- channel agonists
All of the following are mechanisms of action for Antiepileptics EXCEPT:
A. NaV+ channel antagonist
B. Ca2+ channel antagonist
C. Cl- channel antagonist
D. Cl- channel agonist
C. Cl- channel antagonist
Which of the following is an antiepileptic drug w/ a mechanism of action at the GABA-A receptor modulator?
A. Clonidine
B. Zolpidem
C. Phenobarbital
D. Flumazenil
E. All of the above
C. Phenobarbital
Discuss Phenobarbital:
- What is Phenobarbital used to tx?
- What is the mechanism of action?
- What are the adverse effects of Phenobarbital?
Phenobarbital
- Antiepileptic
- GABA-A modulators
- Adverse effects:
- induction of liver enzymes —> a lot of potential for drug/drug interactions
- sedation
- hepatic toxicity
- Osteomalacia
- Respiratory depression
Which of the following has a lot of potential for drug/drug interactions due to the induction of liver enzymes?
A. Clonidine
B. Zolpidem
C. Phenobarbital
D. Flumazenil
E. All of the above
C. Phenobarbital
Which of the following is a NaV+ antagonist used to tx epilepsy?
A. Clonidine
B. Zolpidem
C. Phenobarbital
D. Flumazenil
E. Phenytoin
E. Phenytoin
Discuss Phenytoin:
- What type of drug is Phenytoin?
- What is the mechanism of action for Phenytoin?
- Sometimes also used for _______.
- Why is Phenytoin dangerous?
- What are adverse effects of Phenytoin?
Phenytoin
- Antiepileptic
- NaV+ antagonist
- Sometimes also used for trigeminal neuralgia
- Phenytoin is dangerous bc it is often eliminated by “Zero-order kinetics”
- this means their is a potential for overdose
- Adverse effects:
- Gingival hyperplasia
- can get drug/drug interactions from liver metabolism
Which of the following is eliminated by “Zero-order kinetics” w/ a potential for overdose?
A. Phenytoin
B. Phenobarbital
C. Primidone
D. Carbamazepine
E. Gabapentin
A. Phenytoin
Valproic acid (Valproate) = GABA agonist, NaV+ and CaV2+ antagonist
Phenobarbital = GABA-A
Primidone = metabolized to phenobarbital
Carbamazepine = NaV+ antagonist
Gabapentin = unkown mechanism of action
Phenytoin = NaV+ antagonist
Which of the following may cause gingival hyperplasia?
A. Phenytoin
B. Phenobarbital
C. Primidone
D. Carbamazepine
E. Gabapentin
A. Phenytoin
Valproic acid (Valproate) = GABA agonist, NaV+ and CaV2+ antagonist
Phenobarbital = GABA-A
Primidone = metabolized to phenobarbital
Carbamazepine = NaV+ antagonist
Gabapentin = unkown mechanism of action
Phenytoin = NaV+ antagonist
Which of the following is a NaV+ antagonist used to tx epilepsy?
A. Valproic acid (Valproate)
B. Phenobarbital
C. Primidone
D. Carbamazepine
E. Gabapentin
D. Carbamazepine
Valproic acid (Valproate) = GABA agonist, NaV+ and CaV2+ antagonist
Phenobarbital = GABA-A
Primidone = metabolized to phenobarbital
Carbamazepine = NaV+ antagonist
Gabapentin = unkown mechanism of action
Which of the following is a GABA-A receptor modulator used to tx epilepsy?
A. Valproic acid (Valproate)
B. Phenobarbital
C. Primidone
D. Carbamazepine
E. Gabapentin
B. Phenobarbital
Valproic acid (Valproate) = GABA agonist, NaV+ and CaV2+ antagonist
Phenobarbital = GABA-A
Primidone = metabolized to phenobarbital
Carbamazepine = NaV+ antagonist
Gabapentin = unkown mechanism of action
Which of the following antiepileptic drugs is metabolized to phenobarbital and has acute systemic and CNS toxicity that tend to limit its use?
A. Valproic acid (Valproate)
B. Phenobarbital
C. Primidone
D. Carbamazepine
E. Gabapentin
C. Primidone
Valproic acid (Valproate) = GABA agonist, NaV+ and CaV2+ antagonist
Phenobarbital = GABA-A
Primidone = metabolized to phenobarbital
Carbamazepine = NaV+ antagonist
Gabapentin = unkown mechanism of action
Which of the following antiepileptics is approved as adjunct for partial seizures but is actually used more to treat neuralgia than epilepsy?
A. Valproic acid (Valproate)
B. Phenobarbital
C. Primidone
D. Carbamazepine
E. Gabapentin
E. Gabapentin
Valproic acid (Valproate) = GABA agonist, NaV+ and CaV2+ antagonist
Phenobarbital = GABA-A
Primidone = metabolized to phenobarbital
Carbamazepine = NaV+ antagonist
Gabapentin = unkown mechanism of action
Which of the following is thought to increase GABA and block NaV+ and CaV++?
A. Valproic acid (Valproate)
B. Phenobarbital
C. Primidone
D. Carbamazepine
E. Gabapentin
A. Valproic acid (Valproate)
Ethosuximide = block CaV2+ for absence seizures
Valproic acid (Valproate) = GABA agonist, NaV+ and CaV2+ antagonist
Phenobarbital = GABA-A
Primidone = metabolized to phenobarbital
Carbamazepine = NaV+ antagonist
Gabapentin = unkown mechanism of action
Which of the following is thought to block CaV2+ and is FFDA approved as adjunct for absence seizures?
A. Valproic acid (Valproate)
B. Phenobarbital
C. Ethosuximide
D. Carbamazepine
E. Gabapentin
C. Ethosuximide
Ethosuximide = block CaV2+ for absence seizures
Valproic acid (Valproate) = GABA agonist, NaV+ and CaV2+ antagonist
Phenobarbital = GABA-A
Primidone = metabolized to phenobarbital
Carbamazepine = NaV+ antagonist
Gabapentin = unkown mechanism of action
Which of the following is FDA approved as adjunct for absence seizures?
A.Ethosuximide
B. Phenobarbital
C. Phenytoin
D. Carbamazepine
E. Gabapentin
A.Ethosuximide
Discuss Parkinson’s Disease:
Parkinson’s Disease
- Characterized by progressive hypokinesia
- loss of voluntary movement
- Tremor at rest
- involuntary hyperkinesia
- “Pill rolling”
- tends to disappear w/ voluntary movement
- Progresses to muscle rigidity
- Patients have “Off” and “On” phases
- Can lead to cognitive impairment
__________ is characterized by a defect in the signaling pathways of the basal ganglia.
Parkinson’s Disease
Parkinson’s disease is characterized by a defect in the signaling pathways of the ______.
basal ganglia
Discuss Parkinson’s disease tx strategies?
Parkinson’s tx strategies
- increase dopamine receptor activation in basal ganglia
- block muscarinic receptors in the basal ganglia
- block NMDA glutamate receptors
In Parkinson’s disease there is a loss of DA cells in the ______.
substantia nigra
- leads to less GABAergic (inhibitory) stimulation of the thalamus
- Get increased excitatory output to the motor cortex
Which of the following is transported past BBB and converted into dopamine to tx Parkinson’s?
A. Carbidopa
B. Levodopa
C. Pramipexole
D. Tolcapone
E. Rasagiline
B. Levodopa
Carbipoba = dopa decarboxylase inhibitor
Levodopa = (L-Dopa), transported pass BBB converted to dopamine
Pramipexole = DA receptor agonist
Tolcapone = block catecholamine O-methyl transferase (COMT)
Rasagiline = blocks monoamine oxidase type B (MAO-B)
Selegiline = similar mechanism to rasagiline
Which of the following is a dopa decarboxylase inhibitor?
A. Carbidopa
B. Levodopa
C. Pramipexole
D. Tolcapone
E. Rasagiline
A. Carbidopa
note: Carbipoa is used in conjunction w/ L-Dopa
Carbipoba = dopa decarboxylase inhibitor
Levodopa = (L-Dopa), transported pass BBB converted to dopamine
Pramipexole = DA receptor agonist
Tolcapone = block catecholamine O-methyl transferase (COMT)
Rasagiline = blocks monoamine oxidase type B (MAO-B)
Selegiline = similar mechanism to rasagiline
Which of the following does NOT pass BBB, keeps L-Dipa from being converted into dopamine in periphery and reduces side effect?
A. Carbidopa
B. Levodopa
C. Pramipexole
D. Tolcapone
E. Rasagiline
A. Carbidopa
Carbipoba = dopa decarboxylase inhibitor
Levodopa = (L-Dopa), transported pass BBB converted to dopamine
Pramipexole = DA receptor agonist
Tolcapone = block catecholamine O-methyl transferase (COMT)
Rasagiline = blocks monoamine oxidase type B (MAO-B)
Selegiline = similar mechanism to rasagiline
Which of the following block catecholamine O-methyl transferase (COMT), which prevents breakdown of dopamine in CNS?
A. Carbidopa
B. Levodopa
C. Pramipexole
D. Tolcapone
E. Rasagiline
D. Tolcapone
Carbipoba = dopa decarboxylase inhibitor
Levodopa = (L-Dopa), transported pass BBB converted to dopamine
Pramipexole = DA receptor agonist
Tolcapone = block catecholamine O-methyl transferase (COMT)
Rasagiline = blocks monoamine oxidase type B (MAO-B)
Selegiline = similar mechanism to rasagiline
Which of the following is a DA receptor agonist used to tx Parkinson’s?
A. Selegiline
B. Levodopa
C. Pramipexole
D. Tolcapone
E. Rasagiline
C. Pramipexole
Carbipoba = dopa decarboxylase inhibitor
Levodopa = (L-Dopa), transported pass BBB converted to dopamine
Pramipexole = DA receptor agonist
Tolcapone = block catecholamine O-methyl transferase (COMT)
Rasagiline = blocks monoamine oxidase type B (MAO-B)
Selegiline = similar mechanism to rasagiline
Which of the following blocks monoamine oxidase type B (MAO-B), which prevents breakdown of dopamine in CNS?
A. Clonidine
B. Levodopa
C. Pramipexole
D. Tolcapone
E. Rasagiline
E. Rasagiline
Carbipoba = dopa decarboxylase inhibitor
Levodopa = (L-Dopa), transported pass BBB converted to dopamine
Pramipexole = DA receptor agonist
Tolcapone = block catecholamine O-methyl transferase (COMT)
Rasagiline = blocks monoamine oxidase type B (MAO-B)
Selegiline = similar mechanism to rasagiline
Which of the following blocks H1 histamine receptors and is used to tx extra-pyramidal side-effects?
A. Amantadine
B. Diphenhydramine
C. Benzotropine
D. Selegiline
B. Diphenhydramine
Which of the following is an anticholinergic drug used to tx parkinson’s?
A. Amantadine
B. Diphenhydramine
C. Benzotropine
D. Selegiline
C. Benzotropine
Which of the following blocks the NMDA receptor and was previously used as an antiflu medication?
A. Amantadine
B. Diphenhydramine
C. Benzotropine
D. Selegiline
A. Amantadine
Amantadine = blocks NMDA receptor (Parkinson’s tx)
Diphenhydramine = blocks H1 receptor
Benzotropine = anticholinergic (tx parkinson’s)
