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Questions and Answers
What critical structural feature is essential for a compound to exhibit selective agonist or antagonist activity at the estrogen receptor?
What critical structural feature is essential for a compound to exhibit selective agonist or antagonist activity at the estrogen receptor?
- An aromatic A-ring combined with a hydroxyl group at the C3 position. (correct)
- A ketone group at the C3 position.
- A bulky alkyl substituent at the C17 position.
- A saturated cyclohexane ring at the A-ring position.
A patient on hormonal birth control experiences breakthrough bleeding. Which alteration in hormone levels is the MOST likely cause?
A patient on hormonal birth control experiences breakthrough bleeding. Which alteration in hormone levels is the MOST likely cause?
- Depressed progestin levels (correct)
- Depressed estrogen levels
- Elevated progestin levels
- Elevated estrogen levels
How do aromatase inhibitors, such as exemestane and letrozole, impact estrogen concentration in the body?
How do aromatase inhibitors, such as exemestane and letrozole, impact estrogen concentration in the body?
- They have no significant impact on estrogen concentration.
- They decrease estrogen concentration by blocking its synthesis. (correct)
- They increase estrogen concentration by preventing its metabolism.
- They increase estrogen concentration by binding to estrogen receptors.
Sulfate-conjugated estrogens offer several advantages over 17β-estradiol. Which of the following is the MOST significant benefit of using sulfate-conjugated estrogens?
Sulfate-conjugated estrogens offer several advantages over 17β-estradiol. Which of the following is the MOST significant benefit of using sulfate-conjugated estrogens?
A patient taking both a Z-drug for insomnia and an antiepileptic drug (AED) is at increased risk for adverse effects due to shared metabolic pathways. What is the primary mechanism underlying this potential drug-drug interaction?
A patient taking both a Z-drug for insomnia and an antiepileptic drug (AED) is at increased risk for adverse effects due to shared metabolic pathways. What is the primary mechanism underlying this potential drug-drug interaction?
Which of the following mechanisms of action is NOT a recognized strategy for antiepileptic drugs (AEDs)?
Which of the following mechanisms of action is NOT a recognized strategy for antiepileptic drugs (AEDs)?
A patient experiencing seizures is prescribed felbamate. What is the MOST relevant mechanism of action of this drug in controlling seizures?
A patient experiencing seizures is prescribed felbamate. What is the MOST relevant mechanism of action of this drug in controlling seizures?
Following the administration of general anesthesia, a patient begins to regain consciousness. Which of the following mechanisms is MOST directly responsible for repolarization of neuronal membranes, leading to the termination of anesthesia-induced effects?
Following the administration of general anesthesia, a patient begins to regain consciousness. Which of the following mechanisms is MOST directly responsible for repolarization of neuronal membranes, leading to the termination of anesthesia-induced effects?
A patient with a known sulfonamide allergy requires a local anesthetic for a minor surgical procedure. Which class of local anesthetics should be avoided due to the risk of cross-sensitivity?
A patient with a known sulfonamide allergy requires a local anesthetic for a minor surgical procedure. Which class of local anesthetics should be avoided due to the risk of cross-sensitivity?
Which of the following factors MOST directly determines the rate at which a local anesthetic diffuses through nerve tissue to reach its site of action?
Which of the following factors MOST directly determines the rate at which a local anesthetic diffuses through nerve tissue to reach its site of action?
A patient experiencing frequent absence seizures requires a medication that selectively blocks T-type calcium channels in thalamic neurons. Which of the following medications is MOST appropriate for this patient?
A patient experiencing frequent absence seizures requires a medication that selectively blocks T-type calcium channels in thalamic neurons. Which of the following medications is MOST appropriate for this patient?
A patient is prescribed a new antiepileptic drug. The doctor mentions that the medication works by enhancing the slow inactivation of sodium channels. Which of the following medications is MOST closely associated with this mechanism of action?
A patient is prescribed a new antiepileptic drug. The doctor mentions that the medication works by enhancing the slow inactivation of sodium channels. Which of the following medications is MOST closely associated with this mechanism of action?
Which combination of mechanisms would MOST effectively reduce neuronal hyperexcitability that leads to seizures?
Which combination of mechanisms would MOST effectively reduce neuronal hyperexcitability that leads to seizures?
A patient taking ramelteon consistently reports that the medication is ineffective in helping them fall asleep. Which of these suggestions is MOST likely to improve the drug's efficacy?
A patient taking ramelteon consistently reports that the medication is ineffective in helping them fall asleep. Which of these suggestions is MOST likely to improve the drug's efficacy?
A patient presents with a suspected benzodiazepine overdose. Which of the following is the MOST appropriate treatment strategy, and why is it preferred over treatments for barbiturate overdose?
A patient presents with a suspected benzodiazepine overdose. Which of the following is the MOST appropriate treatment strategy, and why is it preferred over treatments for barbiturate overdose?
The structure of zolpidem features an imidazopyridine ring. How many nitrogen atoms are contained within this structure?
The structure of zolpidem features an imidazopyridine ring. How many nitrogen atoms are contained within this structure?
Following a traumatic brain injury, a patient exhibits symptoms indicative of a GABA deficiency. Supplementation with which amino acid could MOST directly support GABA synthesis in this patient?
Following a traumatic brain injury, a patient exhibits symptoms indicative of a GABA deficiency. Supplementation with which amino acid could MOST directly support GABA synthesis in this patient?
During the synthesis of catecholamines, which enzyme catalyzes the conversion of L-dopa to dopamine?
During the synthesis of catecholamines, which enzyme catalyzes the conversion of L-dopa to dopamine?
A researcher is investigating the effects of a novel compound on neuronal excitability. The compound increases the activity of GABA but also blocks calcium channels Which of the following antiepileptic medications exhibits a similar dual mechanism of action?
A researcher is investigating the effects of a novel compound on neuronal excitability. The compound increases the activity of GABA but also blocks calcium channels Which of the following antiepileptic medications exhibits a similar dual mechanism of action?
A patient with epilepsy is being treated with multiple medications, including one that blocks NMDA receptors. Which of the following potential side effects is MOST closely associated with NMDA receptor blockade?
A patient with epilepsy is being treated with multiple medications, including one that blocks NMDA receptors. Which of the following potential side effects is MOST closely associated with NMDA receptor blockade?
Flashcards
GABA Activators
GABA Activators
Drugs that enhance GABA activity in the brain to reduce seizures.
GABA Inhibitors
GABA Inhibitors
Drugs that inhibit GABA, potentially increasing seizures.
NMDA Blockers
NMDA Blockers
Medications that block NMDA receptors to prevent excitatory activity.
Calcium Channel Blockade
Calcium Channel Blockade
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Sodium Channel Blockade
Sodium Channel Blockade
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Lacosamide
Lacosamide
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Lamotrigine
Lamotrigine
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Levetiracetam
Levetiracetam
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Flumazenil
Flumazenil
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Catecholamine Synthesis
Catecholamine Synthesis
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Synthesis of GABA
Synthesis of GABA
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Buspirone
Buspirone
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Select Non-steroidal Androgen Receptor Antagonists
Select Non-steroidal Androgen Receptor Antagonists
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Estrogen Receptor Agonists
Estrogen Receptor Agonists
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Aromatase Inhibitors
Aromatase Inhibitors
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Mechanisms of Depolarization
Mechanisms of Depolarization
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Local Anesthetics: Esters vs Amides
Local Anesthetics: Esters vs Amides
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Fatal Local Anesthetic IV
Fatal Local Anesthetic IV
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CYP3A4 Drug Interactions
CYP3A4 Drug Interactions
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Estrogen Overdose Effects
Estrogen Overdose Effects
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Study Notes
Antiepileptic Strategies and Drugs
- GABA Activation: Benzodiazepines (pam/lam), Phenobarbital, Primidone, Levetiracetam
- GABA Inhibition: Tiagabine, Vigabatrin
- NMDA Blockade: Felbamate, Topiramate
- Calcium Channel Blockade: Oxcarbazepine, Levetiracetam, Pregabalin, Gabapentin, Ethosuximide
- Sodium Channel Blockade: Carbamazepine, Oxcarbazepine, Phenytoin, Fosphenytoin, Lamotrigine, Valproate, Zonisamide, Lacosamide, Topiramate
Drugs with Multiple Mechanisms of Action (MOA)
- Lacosamide: Enhances slow inactivation of sodium channels.
- Lamotrigine: Blocks sodium channels and affects calcium channels.
- Levetiracetam: GABA activator and blocks calcium channels.
Strategies to Block Neuronal Hyperexcitability
- Sodium Channel Blockade: Prevents depolarization.
- Calcium Channel Blockade: Prevents depolarization.
- Glutamate Receptor Inhibition: Targets stimulatory neurotransmitter.
- GABA Activity Enhancement: Targets inhibitory neurotransmitter.
- Potassium Channel Opening: Promotes hyperpolarization.
Ramelteon Administration
- Avoid high-fat meals.
- Take 30 minutes before bedtime.
- Melatonin analog for insomnia.
Benzodiazepine Overdose Treatment
- Treatment: Flumazenil (competitive BZD agonist at GABAa receptors).
- Reason: Barbituates lack a specific antagonist; they bind differently on GABAa receptors.
Parent Structures of Z-Drugs
- Zolpidem: Imidazopyridine (2 nitrogens).
- Zaleplon: Pyrazolopyrimidine (3 nitrogens).
- Eszopiclone: Cyclopyrrolone (4 nitrogens).
Neurotransmitter Synthesis Precursors
- Epinephrine, Norepinephrine, Dopamine: Tyrosine
- Serotonin: Tryptophan
- GABA: Glutamate
- Glutamate: Glutamine
Catecholamine Synthesis
- Tyrosine → L-DOPA (Tyrosine hydroxylase).
- L-DOPA → Dopamine (Aromatic amine decarboxylase).
- Dopamine → Norepinephrine (Dopamine beta hydroxylase or COMT).
- Norepinephrine → Epinephrine.
GABA Synthesis
- Glutamate → GABA (Glutamate decarboxylase).
Buspirone
- Anxiolytic: Does not act on GABAa receptors.
- Mechanism: 5-HT1A and 5-HT2 receptor agonist, some affinity for D2 receptors.
- Metabolism: CYP3A4.
- Onset: Longer.
- Drug Interactions: MAOIs, CYP3A4 inhibitors/inducers, serotonergic agents.
Spironolactone Drug Interactions
- NSAIDs
- ARBs
- ACE-Is
Non-Steroidal Androgen Receptor Antagonists
- Drugs: Flutamide, Apalutamide, Bicalutamide, Nilutamide.
- Use: Prostate cancer (combined with GnRH).
- Adverse Effects: Liver toxicity.
- Route: Oral, parenteral, transdermal.
Estrogen Receptor Agonist/Antagonist Requirements
- Aromatic A ring and C3-OH
- C17-OH
- Fluvestrant: Antagonist.
Hormonal Contraceptive Adverse Effects
- High Estrogen: Thromboembolic risk, breakthrough bleeding, stroke, vaginal dryness.
- Low Estrogen: Fibroid growth.
- High Progestin: Decreased libido, acne, hirsutism, jaundice.
- Low Progestin: Breakthrough bleeding.
Estrogen and Progesterone Receptor Agonists Indications
- Estrogen Receptor (ER) Agonists: Tamoxifen, Toremifene, Raloxifene, Bazedoxifene
- Use: Bone agonist, breast tissue antagonist (cancer).
- Progesterone Receptor (PR) Agonists: Uses in hormonal contraception.
Aromatase Inhibitor Effect on Estrogen
- Effect: Decreases estrogen concentration (e.g., Exemestane, Anastrazole, Letrozole).
Selective Estrogen Receptor Modulators (SERMs)
- Mechanism: Antagonist in breast tissue, agonist in bones.
- Examples: Tamoxifen, Toremifene, Raloxifene, Bazedoxifene.
Sulfate-Conjugated Estrogens Advantages
- Longer half-life
- Higher bioavailability
- More stable & predictable
Z-Drug and AED Drug Interactions
- Z-Drugs: CYP3A4 inhibitors/inducers, tobacco smoking, CNS depressants(benzos).
- AEDs: CYP3A4 inhibitors/inducers, benzos , CNS depressants.
AED Mechanism of Action
- Sodium channel blockade
- GABAergic transmission enhancement
- Calcium channel blockade
- Glutamate receptor blockade
NMDA Receptor Blockade in Epilepsy
- Drugs: Felbamate, Topiramate
Depolarization/Hyperpolarization Mechanisms
- Depolarization: Sodium channel opening.
- Repolarization: Sodium channels close, potassium channels open.
- Hyperpolarization: Potassium channels remain open after potential reaches resting level.
Anesthesia Drugs (General)
- Inhaled: Nitrous oxide, Desflurane, Enflurane, Halothane, Isoflurane, Sevoflurane
- Adverse Effects: Cerebral blood flow and ICP.
- IV: Methohexital, Midazolam, Diazepam, Propofol, Ketamine, Etomidate.
Local Anesthetics
- Esters: Benzocaine, Cocaine, Procaine
- Amides: Articaine, Bupivacaine, Lidocaine, Mepivacaine, Prilocaine, Ropivacaine.
Local Anesthetics Lipophilicity and Diffusibility
- Lipophilicity directly correlates with diffusability.
Local Anesthetic Contraindications Related to Antibiotics
- Ester-type local anesthetics: Sulfonamide antibiotics (PABA metabolite formation).
- Aminoglycoside antibiotics: Can enhance neuromuscular blockade.
Fatal IV Local Anesthetic
- Bupivacaine
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