Neuro - Pharmacology Flashcards
Which two -agonists are used to treat glaucoma?
Epinephrine and brimonidine
How do β-agonists treat glaucoma?
They decrease aqueous humor synthesis
Which β-agonist is contraindicated for closed-angle glaucoma?
Epinephrine
Which β-blockers are used to treat glaucoma?
Timolol, betaxolol, carteolol
By what mechanism do β-blockers treat glaucoma?
They decrease aqueous humor secretion
How does acetazolamide treat glaucoma?
It decreases aqueous humor secretion by inhibiting carbonic anhydrase
Which four cholinomimetics are used to treat glaucoma?
Pilocarpine, carbachol, physostigmine, echothiophate
By what mechanism do cholinomimetics treat glaucoma?
They increase outflow of aqueous humor, contract the ciliary muscle, and open the trabecular meshwork
Which drug is used for glaucoma in emergencies?
Pilocarpine
Which prostaglandin increases the outflow of aqueous humor in glaucoma? Of which prostaglandin is it an analogue?
Latanoprost; prostaglandin F2
A patient;s new glaucoma drug is causing browning of the iris. What is she taking?
Latanoprost
Morphine, fentanyl, codeine, heroin, methadone, meperidine, and dextromethorphan are in which category of drugs?
Opioid analgesics
What is the mechanism of action of opioid analgesics?
They act as agonists at the mu, delta, and kappa opioid receptors to modulate synaptic transmission
Match the following substances with the opioid receptor (mu/delta/kappa) that they bind most avidly: morphine, dynorphin, enkephalin.
Dynorphin is avidly bound to the kappa receptor, enkephalin is avidly bound to the delta receptor, and morphine is avidly bound to the mu receptor
Which opioid agonist is used for cough suppression?
Dextromethorphan
Which two opioid agonists are used to alleviate diarrhea?
Loperamide and diphenoxylate
Which opioid analgesic is used for maintenance programs for heroin addicts?
Methadone
What changes in neurotransmitter release result from opioid receptor agonists?
They inhibit release of acetylcholine, norepinephrine, serotonin, glutamate, and substance P
A patient well-known to the emergency department presents with respiratory depression, constipation, and miosis. What is the most likely cause of her condition?
Opioid toxicity
Despite requiring increasing doses for recreational use, which two adverse effects of opioid use will patients not develop tolerance to?
Miosis and constipation
Which two drugs are used to treat opioid toxicity?
Naloxone or naltrexone (opioid receptor antagonists)
Butorphanol acts a partial _____ (agonist/antagonist) at opioid _____ (mu/kappa) receptors, and an _____ (agonist/antagonist) at _____ (kappa/delta) receptors.
Agonist; mu; agonist; kappa
What is the toxicity of butorphanol?
Withdrawal if a patient is on a full opioid agonist, due to its partial agonist activity
What is the benefit of butorphanol over other opioid analgesics?
Butorphanol causes less respiratory depression than full agonists
Which analgesic drug is a weak opioid agonist and inhibitor of serotonin and norepinephrine uptake?
Tramadol
What is the toxic effect of tramadol?
Decreases seizure threshold
What is the clinical use of tramadol?
Chronic pain
Which types of seizures are treated with phenytoin? What is its mechanism of action?
Simple and complex partial seizures, tonic-clonic seizures, and status epilepticus; inactivates sodium channels
Which types of seizures are treated with carbamazepine? What is its mechanism of action?
Simple and complex partial seizures and tonic-clonic generalized seizures; inactivates sodium channels
Which types of seizures are treated with lamotrigine? What is its mechanism of action?
Simple and complex partial seizures and tonic-clonic generalized seizures; inactivates sodium channels
Which types of seizures are treated with gabapentin? What is its mechanism of action?
Simple and complex partial seizures and tonic-clonic generalized seizures; inactivates calcium channels
Which epilepsy drug is the first-line agent used to treat pregnant patients?
Phenobarbital
Which types of seizures are treated with phenobarbital? What is its mechanism of action?
Simple and complex partial seizures and tonic-clonic generalized seizures; increases GABAAaction
What is the first-line agent used to prevent seizures in patients with eclampsia?
Magnesium sulfate
Which types of seizures are treated with valproic acid? What is its mechanism of action?
Simple and complex partial seizures and tonic-clonic and absence generalized seizures; inactivates sodium channels, increases GABA concentration
If magnesium sulfate fails to prevent seizures in a patient with eclampsia, what class of drugs could also be used?
Benzodiazepines
Which types of seizures are treated with ethosuximide? What is its mechanism of action?
Absence generalized seizures; blocks thalamic T-type calcium channels
Which types of seizures are treated with benzodiazepines? What is the mechanism of action?
Status epilepticus; increase the action of GABAA
Which types of seizures are treated with tiagabine? What is its mechanism of action?
Simple and complex partial seizures; inhibits GABA reuptake
Which types of seizures are treated with vigabatrin? What is its mechanism of action?
Simple and complex partial seizures; it irreversibly inhibits GABA transaminase, thus increasing GABA concentration
Which types of seizures are treated with levetiracetam? What is its mechanism of action?
Simple and complex partial seizures and tonic-clonic generalized seizures; its mechanism is unknown, but it may modulate GABA and glutamate release
Which two blood dyscrasias are associated with carbamazepine toxicity?
Agranulocytosis and aplastic anemia
Which two epilepsy drugs may predispose individuals who are taking them to Stevens-Johnson syndrome?
Ethosuximide and lamotrigine
Which antiepileptic drug may cause sedation, tolerance, and dependence in addition to inducing cytochrome P450 enzymes?
Phenobarbital
What epilepsy drug may cause lupus-like syndrome and gingival hyperplasia?
Phenytoin
A patient with epilepsy presents with hirsutism, megaloblastic anemia, ataxia, and gingival hyperplasia. What drug may this person be taking to help treat the epilepsy?
Phenytoin
What are the adverse effects of carbamazepine use?
Diplopia, ataxia, blood dyscrasias, liver toxicity, teratogenesis, and the induction of cytochrome P450
Name the toxicities of ethosuximide; use the mnemonic, EFGH.
Ethosuximide = Fatigue, GI distress, Headache
Acute hepatotoxicity is associated with which antiepileptic drug?
Valproic acid
Women of childbearing age who are using which two antiepileptic drugs should also be using birth control because of the teratogenic risks?
Valproic acid, which causes neural tube defects, and carbamazepine
Which antiepileptic drug is associated with kidney stones and weight loss?
Topiramate
Name two adverse effects of gabapentin.
Sedation and ataxia
What is Stevens-Johnson syndrome?
A disorder characterized by a prodrome of malaise and fever followed by rapid onset of erythematous and purpuric macules found on oral, ocular, and genital surfaces that eventually progress to epidermal necrosis and the sloughing of skin
What is the mechanism of action of phenytoin?
Phenytoin creates a use-dependent blockade of sodium channels and inhibits glutamate release from excitatory presynaptic neurons
What is the teratogenic effect of phenytoin use during pregnancy?
Fetal hydantoin syndrome
Which antiepileptic drug is primarily used to treat tonic-clonic seizures and is also a class IB antiarrhythmic agent?
Phenytoin
A patient presents with nystagmus, ataxia, diplopia, and sedation after starting an antiepileptic drug for tonic-clonic seizures. What medication was the patient most likely started on?
Phenytoin
Phenobarbital, pentobarbital, thiopental, and secobarbital are members of which class of drugs?
Barbiturates
True or False? Dependence is a major adverse effect of barbiturates.
True