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131 Cards in this Set
- Front
- Back
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What is the effect of drugs that treat glaucoma? |
Decrease intraocular pressure (IOP) via ↓ in amount of aqueous humor (inhibits synthesis / secretion or ↑ drainage)
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What are the types of drugs to treat glaucoma?
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- α-agonists: Epinephrine and Brimonidine (α2)
- β-blockers: Timolol, Betaxolol, Carteolol - Diuretics: Acetazolamide - Cholinomimetics: direct (pilocarpine and carbachol) - Cholinomimetics: indirect (physostigmine and echothiophate) - Prostaglandin: Latanoprost (PGF2α) |
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Drugs to treat glaucoma act how on α receptors? Which drugs?
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α-Agonists:
- Epinephrine - Brimonidine (α2) |
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What is the mechanism and side effects of using Epinephrine to treat glaucoma?
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- Mechanism: ↓ aqueous humor synthesis via vasoconstriction (α-agonist)
- Side effects: Mydriasis (dilation); do not use in closed-angle glaucoma |
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What is the mechanism and side effects of using Brimonidine to treat glaucoma?
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- Mechanism: ↓ aqueous humor synthesis via α2 agonism
- Side effects: blurry vision, ocular hyperemia, foreign body sensation, ocular allergic reactions, ocular pruritus |
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Drugs to treat glaucoma act how on β receptors? Which drugs?
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β-Blockers
- Timolol - Betaxolol - Carteolol |
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What is the mechanism and side effects of using Timolol, Betaxolol, and Carteolol to treat glaucoma?
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- Mechanism: ↓ aqueous humor synthesis via β-blockade
- Side effects: no pupillary or vision changes |
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What diuretic can be used to treat glaucoma?
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Acetazolamide
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What is the mechanism and side effects of using Acetazolamide to treat glaucoma?
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- Mechanism: ↓ aqueous humor synthesis via inhibition of carbonic anhydrase
- Side effects: no pupillary or vision changes |
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What cholinomimetic drugs can be used to treat glaucoma?
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- Direct: Pilocarpine, Carbachol
- Indirect: Physostigmine, Echothiophate |
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What is the mechanism and side effects of using Pilocarpine and Carbachol to treat glaucoma?
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- Mechanism: direct cholinomimetics → ↑ outflow of aqueous humor via contraction of ciliary muscles and opening of trabecular meshwork
- Side effects: miosis and cyclospasm (contraction of ciliary muscle |
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What is the mechanism and side effects of using Physostigmine and Echothiophate to treat glaucoma?
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- Mechanism: direct cholinomimetics → ↑ outflow of aqueous humor via contraction of ciliary muscles and opening of trabecular meshwork
- Side effects: miosis and cyclospasm (contraction of ciliary muscle |
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Which drug can you use in glaucoma emergencies? Why?
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Pilocarpine - very effective at opening meshwork into canal of Schlemm
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What prostaglandin drug can be used to treat glaucoma?
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Latanoprost (PGF-2α)
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What is the mechanism and side effects of using Latanoprost to treat glaucoma?
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- Mechanism: prostaglandin (PGF-2α) → ↑ outflow of aqueous humor
- Side effects: darkens color of iris (browning) |
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What drugs treat glaucoma by decreasing aqueous humor synthesis?
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- α-Agonists: Epinephrine and Brimonidine (α2)
- β-Blockers: Timolol, Betaxolol, Carteolol - Diuretics: Acetazolamide |
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What drugs treat glaucoma by increasing outflow of aqueous humor?
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- Direct Cholinomimetics: Pilocarpine and Carbachol
- Indirect Cholinomimetics: Physostigmine and Echothiophate - Prostaglandin: Latanoprost (PGF-2α) |
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What drug has the side effect of darkening the color of the iris (browning)?
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Latanoprost (PGF-2α) - prostaglandin used to ↑ outflow of aqueous humor
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What are the opioid analgesics?
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- Morphine
- Fentanyl - Codeine - Loperamide - Methadone - Meperidine - Dextromethorphan - Diphenoxylate |
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What is the mechanism of opioid analgesics?
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- Act as agonists at opioid receptors to modulate synapatic transmission
- Opens K+ channels, closes Ca2+ channels → ↓ synaptic transmission - Inhibits release of ACh, NE, 5-HT, glutamate, and substance P |
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What acts at the µ (mu) opioid receptor?
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Morphine
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What acts at the δ (delta) opioid receptor?
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Enkephalin
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What acts at the κ (kappa) opioid receptor?
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Dynorphin
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How do opioid analgesics modulate synaptic transmission?
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- Opens K+ channels
- Closes Ca2+ channels - ↓ Synaptic transmission - Inhibits release of ACh, NE, 5-HT, Glutamate, and Substance P |
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What are the clinical uses of opioid analgesics?
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- Pain
- Cough suppression (dextromethorphan) - Diarrhea (loperamide and diphenoxylate) - Acute pulmonary edema - Maintenance programs for heroin addicts (methadone) |
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What opioid can be used for cough suppression?
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Dextromethorphan
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What opioid can be used for diarrhea?
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- Loperamide
- Diphenoxylate |
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What opioid can be used in maintenance programs for heroin addicts?
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Methadone
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What are the possible side effects of opioids?
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- Addiction
- Respiratory depression - Constipation - Miosis (pinpoint pupils) - Addictive CNS depression with other drugs |
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What are the characteristics of tolerance to opioids?
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Tolerance does not develop to miosis and constipation
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How do you treat opioid toxicity?
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Naloxone or Naltrexone (opioid receptor antagonist)
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What are the partial opioid agonists?
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- Butorphanol
- Tramadol |
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What is the mechanism of Butorphanol?
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- Mu-opioid receptor partial agonist
- Kappa-opioid receptor agonist - Produces analgesia |
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What is the clinical use of Butorphanol? What is the benefit of this drug over other opioids?
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- Severe pain (migraine, labor, etc)
- Causes less respiratory depression than full opioid agonists because it is only a partial mu-opioid agonist |
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What are the side effects / limitations of Butorphanol?
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- Opioid withdrawal symptoms if patient is also taking full opioid agonist (competition for receptors and this drug is only a partial agonist - so acts like antagonist compared to full agonist)
- Overdose not easily reversed with naloxone |
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What is the mechanism of Tramadol?
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- Very week opioid agonist
- Also inhibits serotonin and NE reuptake (works on multiple NTs - "tram it all" in with "tramadol") |
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What are the clinical uses of Tramadol? Side effects?
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- Used for chronic pain
- Side effects: similar to opioids, decreases seizure threshold, serotonin syndrome |
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Which opioid can cause serotonin syndrome? Why?
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Tramadol - it also inhibits serotonin and NE reuptake in addition to its week opioid agonistic activity
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What drugs work for simple partial seizures? Which is first line?
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** Carbamazepine = First-Line
- Phenytoin - Valproic acid - Gabapentin - Phenobarbital - Topiramate - Lamotrigine - Levetiracetam - Tiagabine - Vigabatrin (Same as for simple partial seizures) |
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What drugs work for complex partial seizures? Which is first line?
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** Carbamazepine = First-Line
- Phenytoin - Valproic acid - Gabapentin - Phenobarbital - Topiramate - Lamotrigine - Levetiracetam - Tiagabine - Vigabatrin (Same as for complex partial seizures) |
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What drugs work for generalized tonic-clonic seizures? Which is first line?
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** Phenytoin = First-Line
** Carbamazepine = First-Line ** Valproic Acid = First-Line - Gabapentin - Phenobarbital - Topiramate - Lamotrigine - Levetiracetam |
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What drugs work for generalized absence seizures? Which is first line?
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** Ethosuximide = First-Line
- Valproic acid - Lamotrigene |
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What drugs work for status epilepticus seizures?
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- Benzodiazepines (diazepam and lorazepam): first line for acute
- Phenytoin: first line for prophylaxis |
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What drug is first-line for absence seizures? Mechanism?
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Ethosuximide
- Blocks thalamic T-type Ca2+ channels |
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What are the side effects of Ethosuximide?
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EFGHIJ:
- "Ethosuximide causes Fatigue, GI distress, Headache, Itching, and stevens-Johnson syndrome" - Fatigue - GI problems - Headache - Urticaria (itching) - Steven-Johnson syndrome |
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What drug is first line for acute status epilepticus? Mechanism?
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Benzodiazepines (Diazepam, Lorazepam)
- ↑ GABA-A action |
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What are the uses and side effects of Benzodiazepines (Diazepam and Lorazepam)?
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- Used first line for acute status epilepticus
- Also for eclampsia seizures (1st is MgSO4) - Side effects: sedation, tolerance, dependence, respiratory depression |
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What are the uses of Phenytoin? Mechanism?
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- First line for tonic-clonic seizures
- First line for prophylaxis of status epilepticus - ↑ Na+ channel inactivation, zero-order kinetics |
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What are the side effects of Phenytoin?
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- Nystagmus
- Diplopia - Ataxia - Sedation - Gingival hyperplasia - Hirsutism - Peripheral neuropathy - Megaloblastic anemia - Teratogenesis (fetal hydantoin syndrome) - SLE-like syndrome - Induction of cytochrome P-450 - Lymphadenopathy - Stevens-Johnson syndrome - Osteopenia |
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What form of Phenytoin can be taken for parenteral use?
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Fosphenytoin
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What is Carbamazepine used for? Mechanism?
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First-line for:
- Partial simple seizures - Partial complex seizures - Tonic-clonic seizures - Trigeminal neuralgia Mechanism: - ↑ Na+ channel inactivation |
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What are the side effects of Carbamazepine?
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- Diplopia
- Ataxia - Blood dyscrasias (agranulocytosis, aplastic anemia) - Liver toxicity - Teratogenesis - Induction of cytochrome P-450 - SIADH - Stevens-Johnson syndrome |
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What drug is first line for trigeminal neuralgia?
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Carbamazepine
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What is Valproic Acid used for?
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- First-line for tonic-clonic seizures
- Also for simple partial, complex partial, myoclonic, and absence seizures - Also for bipolar disorder |
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What is the mechanism of Valproic Acid?
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- ↑ Na+ channel inactivation
- ↑ GABA concentration by inhibiting GABA transaminase |
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What are the side effects of Valproic Acid?
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- GI distress
- Rare but fatal hepatotoxicity (measure LFTs) - Neural tube defects in fetus (spina bifida) - Tremor - Weight gain - Contraindicated in pregnancy |
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What is Gabapentin used for? Mechanism?
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Used for:
- Simple partial seizures - Complex partial seizures - Tonic-clonic seizures - Peripheral neuropathy - Post-herpetic neuralgia - Migraine prophylaxis - Bipolar disorder Mechanism: - Primarily inhibits high-voltage-activated Ca2+ channels - Designed as a GABA analog |
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What are the side effects of Gabapentin?
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- Sedation
- Ataxia |
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What is Phenobarbital used for? Mechanism?
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Used for:
- Simple partial seizures - Complex partial seizures - Tonic-clonic seizures - 1st line in neonates Mechanism: - ↑ GABA-A action |
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What are the side effects of Phenobarbital?
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- Sedation
- Tolerance - Dependence - Induction of cytochrome P-450 - Cardiorespiratory depression |
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What is Topiramate used for? Mechanism?
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Used for:
- Simple partial seizures - Complex partial seizures - Tonic-clonic seizures - Also used for migraine prevention Mechanism: - Blocks Na+ channels, ↑ GABA action |
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What are the side effects of Topiramate?
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- Sedation
- Mental dulling - Kidney stones - Weight loss |
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What is Lamotrigine used for? Mechanism?
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Used for:
- Simple partial seizures - Complex partial seizures - Tonic-clonic seizures - Absence seizures Mechanism: - Blocks voltage-gated Na+ channels |
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What are the side effects of Lamotrigine?
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Stevens-Johnson Syndrome (must be titrated slowly)
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What is Levetiracetam used for? Mechanism?
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Used for:
- Simple partial seizures - Complex partial seizures - Tonic-clonic seizures Mechanism: - Unknown, may modulate GABA and glutamate release |
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What is Tiagabine used for? Mechanism?
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Used for:
- Simple partial seizures - Complex partial seizures Mechanism: - ↑ GABA by inhibiting re-uptake |
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What is Vigabatrin used for? Mechanism?
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Used for:
- Simple partial seizures - Complex partial seizures Mechanism: - ↑ GABA by irreversibly inhibiting GABA transaminase |
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What is Stevens-Johnson Syndrome?
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- Prodrome of malaise and fever followed by rapid onset of erythematous / purpuric macules (oral, ocular, genital)
- Skin lesions progress to epidermal necrosis and sloughing |
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Which epilepsy medications cause Stevens-Johnson Syndrome?
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- Ethosuximide
- Phenytoin - Carbamazepine - Lamotrigine |
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Which epilepsy medication causes gingival hyperplasia?
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Phenytoin
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Which epilepsy medication causes hirsutism?
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Phenytoin
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Which epilepsy medication causes SLE like syndrome?
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Phenytoin
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Which epilepsy medication causes blood dyscrasias?
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Carbamazepine
Blood dyscrasias: - Agranulocytosis - Aplastic anemia |
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Which epilepsy medication causes neural tube defects?
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Valproic acid
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Which epilepsy medication causes kidney stones?
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Topiramate
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Which epilepsy medication causes induction of cytochrome P-450?
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- Phenytoin
- Phenobarbital |
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Which epilepsy medication is used for peripheral neuropathy?
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Gabapentin
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Which epilepsy medication is used for post-herpetic neuralgia?
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Gabapentin
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Which epilepsy medication is used for migraine prophylaxis?
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- Gabapentin
- Topiramate |
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Which epilepsy medication is used for bipolar disorder?
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- Valproic acid
- Gabapentin |
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Which epilepsy medication is used first line for neonates?
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Phenobarbital
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What are the types of barbiturates?
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- Phenobarbital
- Pentobarbital - Thiopental - Secobarbital |
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What is the mechanism of barbiturates?
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- Facilitate GABA-A actation by ↑ duration of Cl- channel opening
- ↓ Neuron firing → ↑ duration - Contraindicated in porphyria |
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In what condition are barbiturates contraindicated?
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Porphyria
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What are the clinical uses of barbiturates?
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- Sedative for anxiety
- Seizures - Insomnia - Induction of anesthesia (thiopental) |
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What are the possible side effects of barbiturates?
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- Respiratory and cardiovascular depression (can be fatal)
- CNS depression (can be exacerbated by EtOH use) - Dependence - Drug interactions (induces cytochrome P-450) |
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How do you treat an overdose of barbiturates?
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Supportive - assist respiration and maintain BP
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What are the types of benzodiazepines?
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- Diazepam
- Lorazepam - Triazolam - Temazepam - Oxazepam - Midazolam - Chlordiazepoxide - Alprazolam |
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What is the mechanism of benzodiazepines?
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- Facilitate GABA-A action by ↑ frequency of Cl- channel opening
- ↓ REM sleep |
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Which benzodiazepines are short-acting? Implications?
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Higher addictive potential
- Triazolam - Oxazepam - Midazolam |
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Which benzodiazepines are longer-acting? Implications?
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Less addictive potential
- Diazepam - Lorazepam - Temazepam - Chlordiazepoxide - Alprazolam |
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What drugs bind the GABA-A receptor?
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Ligand-gated Cl- channel:
- Benzodiazepines - Barbiturates - EtOH |
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What are the clinical uses of benzodiazepines?
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- Anxiety
- Spasticity - Status epilepticus (lorazepam and diazepam) - Detoxification (especially alcohol withdrawal - DTs) - Night terrors - Sleep-walking - General anesthetic (amnesia, muscle relaxation) - Hypnotic (insomnia) |
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What are the side effects of benzodiazepines?
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- Dependence
- Addictive CNS depression effects with alcohol - Less risk of respiratory depression and coma than with barbiturates |
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How do you treat an overdose of benzodiazepines?
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Flumazenil (competitive antagonist at GABA benzodiazepine receptor)
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What are the non-benzodiazepine hypnotics?
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All ZZZs put you to sleep:
- Zolpidem (Ambien) - Zaleplon - EsZopiclone |
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What is the mechanism and clinical uses of non-benzodiazepine hypnotics?
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- Act via the BZ1 subtype of the GABA receptor
- Used for insomnia |
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What are the side effects of non-benzodiazepine hypnotics?
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- Ataxia
- Headaches - Confusion - Short duration because of rapid metabolism by liver enzymes - Unlike other sedative-hypnotics, cause only modest day-after psychomotor depression and few amnestic effects - ↓ Dependence risk than benzodiazepines |
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What are the characteristics of CNS drugs?
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CNS drugs must be lipid soluble (cross the blood-brain barrier) or be actively transported
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How does the blood and lipid solubility affect anesthetics?
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- Drugs with ↓ solubility in blood → rapid induction and recovery times
- Drugs with ↑ solubility in lipids → ↑ potency → 1/MAC |
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What is the MAC?
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Minimal Alveolar Concentration (of inhaled anesthetic) required to prevent 50% of subjects from moving in response to noxious stimulus (eg, skin incision)
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What property makes an anesthetic have rapid induction and recovery times?
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Drugs with ↓ solubility in blood
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What property makes an anesthetic have increased potency?
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Drugs with ↑ solubility in lipids
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What are the types of inhaled anesthetics?
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- Halothane
- Enflurane - Isoflurane - Sevoflurane - Methoxyflurane - Nitrous oxide |
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What are the effects of inhaled anesthetics?
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- Myocardial depression
- Respiratory depression - Nausea / emesis - ↑ Cerebral blood flow (↓ cerebral metabolic demand) |
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Which inhaled anesthetic causes hepatotoxicity?
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Halothane
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Which inhaled anesthetic causes nephrotoxicity?
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Methoxyflurane
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Which inhaled anesthetic causes proconvulsant?
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Enflurane
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Which inhaled anesthetic causes expansion of trapped gas in a body cavity?
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Nitrous Oxide
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What toxic side effect can all inhaled anesthetics cause?
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Malignant hypertension - rare, life-threatening hereditary condition in which inhaled anesthetics (except nitrous oxide) and succinylcholine induce fever and severe muscle contractions
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How do you treat malignant hypertension?
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Dantrolene
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What are the types of IV anesthetics?
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- Barbiturates: Thiopental
- Benzodiazepines: Midazolam - Arylcyclohexylamines (ketamine) - Opioids - Propofol |
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Which IV anesthetic is high potency and high lipid solubility? Implications?
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Barbiturates (Thiopental)
- Rapid entry into brain - Rapid redistribution |
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What is Thiopental used for?
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- Induction of anesthesia
- Short surgical procedures |
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What terminates the action of Thiopental?
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Terminated by rapid redistribution into tissue (ie, skeletal muscle) and fat
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What are the negative effects of Thiopental (IV anesthetic)?
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Decreases cerebral blood flow
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What is the most common anesthetic used for endoscopy?
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Midazolam (benzodiazepine IV anesthetic)
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What is Midazolam used for?
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- IV anesthetic used for endoscopy
- Adjunctively used with gaseous anesthetics and narcots |
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What are the negative effects of Midazolam (IV anesthetic)?
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- Post-operative respiratory depression
- ↓ BP - Anterograde amnesia |
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What do you give a patient with overdose on IV Midazolam?
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Flumazenil
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What type of IV anesthetic blocks NMDA receptors?
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Arylcyclohexylamines (Ketamine / PCP analog)
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What is the mechanism of Ketamine?
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- PCP analog
- Dissociative anesthetic - Blocks NMDA receptors |
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What are the effects of Ketamine (IV anesthetic)?
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- Cardiovascular stimulant
- Hallucinations - Bad dreams - ↑ Cerebral blood flow |
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What types of opioids can be used as IV anesthetics?
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- Morphine
- Fentanyl Use with other CNS depressants during general anesthesia |
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What anesthetic can be used for sedation in the ICU? Mechanism?
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Propofol (IV anesthetic) - potentiates GABA-A
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What are the characteristics of Propofol?
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- Rapid anesthesia induction
- Good for short procedures - Less post-op nausea (than thiopental) |
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What are the types of local anesthetics?
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- Esters
- Amides |
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What are the types of ester local anesthetics?
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- Procaine
- Cocaine - Tetracaine |
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What are the types of amide local anesthetics?
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Amides have 2 I's in name
- Lidocaine - Mepivicaine - Bupivacaine |
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What is the mechanism of local anesthetics?
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- Blocks Na+ channels by binding to specific receptors on inner portion of channel
- Preferentially bind to activated Na+ channels, so most effective in rapidly firing neurons |
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How are tertiary amine local anesthetics different from other local anesthetics?
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Penetrate membrane in uncharged form, then bind to ion channels as charged form
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