Pharmacology 1 Flashcards
Do not use in closed-angled glaucoma
Epinephrine
Alpha-2 agonist, decreases aquemous humor synthesis
Brimonidine
Decreases aqueous humor synthesis via vasoconstriction
Epinephrine
Beta-blockers that decrease aqueous humor synthesis
Timolol, Betaxolol, Carteolol
S/E of Brimonidine
blurry vision, ocular hyperemia, foreign body sensation, Ax rxn, ocular pruritis
Diuretic that decreases aqueous humor synthesis via inhibition of carbonic anhydrase
Acetazolamide
S/E of Cholinomimetics on glaucoma
miosis and cyclospasm (contraction of ciliary muscle)
Darkens color of iris (browning)
Latanoprost (PGF2alpha), increases outflow of aqueous humor
Opioid Analgesics
Morphine, Fentanyl, Codeine, Loperamide, Methadone, Meperidine, Dextromethorphan, Diphenoxylate
Open K+ channels, close Ca2+ channels to decrease synaptic transmission and inhibit the release of ACh, NE, 5-HT, glutamate and substance P
Opioids
Morphine receptor
mu
Enkephalin receptor
Delta
Dynorphin receptor
Kappa
Cough Suppression
Dextromethorphan
Opioid to tx Diarrhea
Loperamide and diphenoxylate
Opioid receptor antagonist
Naloxone or Naltrexone
Mu-opiod receptor partial agonist and kappa-opioid receptor agonist; produces analgesia
Butorphanol
Very weak opioid agonist; also inhibits serotonin and NE reuptake
Tramadol
Toxicity of Tramadol
decreases seizure threshold
serotonin syndrome
Blocks thalamic T-type Calcium channels
Ethosuximide
Used for absence seizures
Ethosuximide (sucks to have silent seizures)
1st line (DOC) for acute status epilepticus
Benzodiazepines (diazepam and lorazepam)
1st line for eclampsia seizures
MgSO4
Lamotrigine S/E
Stevens-Johnson Syndrome, so must titrate slowly
1st line prophylaxis for status epilepticus
Phenytoin
First line for simple, complex and tonic-clonic seizures
Carbamazepine
1st line for trigeminal neuralgia
Carbamazepine
Used for peripheral neuropathy, postherpetic neuralgia, migraine prophylaxis, bipolar disorder
Gabapentin
Two direct-acting cholinomimetics that increase aqueous outflow through ciliary muscle
Pilocarpine, carbachol
Two indirect-acting cholinomimetics that increase aqueous outflow through ciliary muscle contraction and opening of trabecular meshwork
Physostigmine, echothiophate
Nonselective alpha agonist that decreases aqueous production
Epinephrine
Common side effect of sedative hypnotics
CNS depression
Occurs when sedative hypnotics are used long-term
Tolerance and physical dependence
Mechanism of action of benzodiazepines
Increase frequency of GABA-mediated chloride ion channel (GABAA) opening
Main route of metabolism for benzodiazepines
Hepatic
Useful side effect of benzodiazepines in patients undergoing stressful procedures or surgery
Anterograde amnesia
Three benzodiazepines that are metabolized only by Phase II conjugation and therefore is useful in elderly patients
Lorazepam, oxazepam, and temazepam
Two benzodiazepines that have active metabolites with long half-lives
Diazepam, chlordiazepoxide
Clinical uses of benzodiazepines
Anxiety, insomnia, alcohol detoxification, status epilepticus, spasticity
Reason why benzodiazepines are safer than barbiturates
Benzodiazepines work only in presence of GABA
Mechanism of action of barbiturates
Increase duration of GABAA chloride channel opening
Most serious side effects of barbiturates
Respiratory and cardiovascular depression
Barbiturates may precipitate this hematologic condition
Porphyria
Barbiturates decrease the effectiveness of many other drugs via this pharmacokinetic property
Induce CYP450
Effect of benzodiazepines and barbiturates on sleep architecture
Suppress REM
Three nonbenzodiazepine hypnotics that lack suppressive effect on REM and are preferred over benzodiazepines for the treatment of insomnia
Zolpidem, zaleplon, eszopiclone
Mechanism of action of zolpidem
Activates BZ1 subtype of GABAA receptor
Antiepileptic drug that can induce CYP450, is teratogenic, and can cause diplopia, ataxia, and blood dyscrasias; follows first order kinetics of elimination
Carbamazepine
Drugs of choice for generalized tonic-clonic seizures
Carbamazepine, phenytoin, valproic acid
Mechanism of action of Phenytoin, Carbamazepine, Lamotrigine
Blocks sodium channels
Antiepileptic agent that exhibits zero-order kinetics, causes fetal hydantoin syndrome, and induces CYP450
Phenytoin
Side effects of phenytoin
Gingival hyperplasia, nystagmus, diplopia and ataxia
Mechanism of action of valproic acid
Blocks sodium channels, T-type calcium channels, and increase GABA concentration
Drug of choice for myoclonic seizures that may also be used for absence seizures
Valproic acid
Antiepileptic drug that can cause fatal hepatotoxicity and neural tube defects
Valproic acid
Antiepileptic drugs that may also be used for bipolar disorder
Valproic acid, carbamazepine, gabapentin
Side effects of these drugs include nausea and vomiting, euphoria, dependence, tolerance, sedation, respiratory depression, constipation
Opioids
Tolerance to all effects of opioid agonists can develop except
Miosis, constipation
Strong opioid agonists
Morphine, methadone, meperidine, and fentanyl
Opioids used in anesthesia
Morphine and fentanyl
Opioid that can be given PO, IV, IM, and intrathecal to relieve anxiety associated with pulmonary edema
Morphine
Opioid available trans-dermally
Fentanyl
Opioid with antimuscarinic activity
Meperidine
Long-acting opioids used in the management of withdrawal states
Methadone, Buprenorphine
Opioid that can cause hyperpyrexic coma with MAOI and serotonin syndrome with SSRI
Meperidine
Moderate opioid agonists
Codeine, hydrocodone, and oxycodone
Partial opioid agonist that has a long duration of action and is resistant to naloxone reversal
Buprenorphine
Opioid antagonist that is given IV
Naloxone
Opioid Antagonist that is given orally
Naltrexone
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