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185 Cards in this Set
- Front
- Back
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? |
- α-agonists: Epinephrine and Brimonidine (α2) |
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Drugs to treat glaucoma act how on α receptors? Which drugs? |
α-Agonists: |
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What is the mechanism and side effects of using Epinephrine to treat glaucoma? |
- Mechanism: ↓ aqueous humor synthesis via vasoconstriction (α-agonist) |
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What is the mechanism and side effects of using Brimonidine to treat glaucoma? |
- Mechanism: ↓ aqueous humor synthesis via α2 agonism |
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Drugs to treat glaucoma act how on β receptors? Which drugs? |
β-Blockers |
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What is the mechanism and side effects of using Timolol, Betaxolol, and Carteolol to treat glaucoma? |
- Mechanism: ↓ aqueous humor synthesis via β-blockade |
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What diuretic can be used to treat glaucoma? |
Acetazolamide |
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What is the mechanism and side effects of using Acetazolamide to treat glaucoma? |
- Mechanism: ↓ aqueous humor synthesis via inhibition of carbonic anhydrase |
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What cholinomimetic drugs can be used to treat glaucoma? |
- Direct: Pilocarpine, Carbachol |
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What is the mechanism and side effects of using Pilocarpine and Carbachol to treat glaucoma? |
- Mechanism: direct cholinomimetics → ↑ outflow of aqueous humor via contraction of ciliary muscles and opening of trabecular meshwork |
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What is the mechanism and side effects of using Physostigmine and Echothiophate to treat glaucoma? |
- Mechanism: direct cholinomimetics → ↑ outflow of aqueous humor via contraction of ciliary muscles and opening of trabecular meshwork |
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Which drug can you use in glaucoma emergencies? Why? |
Pilocarpine - very effective at opening meshwork into canal of Schlemm |
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What prostaglandin drug can be used to treat glaucoma? |
Latanoprost (PGF-2α) |
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What is the mechanism and side effects of using Latanoprost to treat glaucoma? |
- Mechanism: prostaglandin (PGF-2α) → ↑ outflow of aqueous humor |
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What drugs treat glaucoma by decreasing aqueous humor synthesis? |
- α-Agonists: Epinephrine and Brimonidine (α2) |
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What drugs treat glaucoma by increasing outflow of aqueous humor? |
- Direct Cholinomimetics: Pilocarpine and Carbachol |
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What drug has the side effect of darkening the color of the iris (browning)? |
Latanoprost (PGF-2α) - prostaglandin used to ↑ outflow of aqueous humor |
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What are the opioid analgesics? |
- Morphine |
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What is the mechanism of opioid analgesics? |
- Act as agonists at opioid receptors to modulate synaptic transmission |
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What acts at the µ (mu) opioid receptor? |
Morphine |
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What acts at the δ (delta) opioid receptor? |
Enkephalin |
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What acts at the κ (kappa) opioid receptor? |
Dynorphin |
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How do opioid analgesics modulate synaptic transmission? |
- Opens K+ channels |
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What are the clinical uses of opioid analgesics? |
- Pain |
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What opioid can be used for cough suppression? |
Dextromethorphan |
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What opioid can be used for diarrhea? |
- Loperamide |
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What opioid can be used in maintenance programs for heroin addicts? |
Methadone |
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What are the possible side effects of opioids? |
- Addiction |
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What are the characteristics of tolerance to opioids? |
Tolerance does not develop to miosis and constipation |
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How do you treat opioid toxicity? |
Naloxone or Naltrexone (opioid receptor antagonist) |
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What are the partial opioid agonists? |
- Butorphanol |
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What is the mechanism of Butorphanol? |
- Mu-opioid receptor partial agonist |
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What is the clinical use of Butorphanol? What is the benefit of this drug over other opioids? |
- Severe pain (migraine, labor, etc) |
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What are the side effects / limitations of Butorphanol? |
- 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) |
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What is the mechanism of Tramadol? |
- Very week opioid agonist |
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What are the clinical uses of Tramadol? Side effects? |
- Used for chronic pain |
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Which opioid can cause serotonin syndrome? Why? |
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? |
** Carbamazepine = First-Line |
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What drugs work for complex partial seizures? Which is first line? |
** Carbamazepine = First-Line |
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What drugs work for generalized tonic-clonic seizures? Which is first line? |
** Phenytoin = First-Line |
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What drugs work for generalized absence seizures? Which is first line? |
** Ethosuximide = First-Line |
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What drugs work for status epilepticus seizures? |
- Benzodiazepines (diazepam and lorazepam): first line for acute |
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What drug is first-line for absence seizures? Mechanism? |
Ethosuximide |
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What are the side effects of Ethosuximide? |
EFGHIJ: |
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What drug is first line for acute status epilepticus? Mechanism? |
Benzodiazepines (Diazepam, Lorazepam) |
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What are the uses and side effects of Benzodiazepines (Diazepam and Lorazepam)? |
- Used first line for acute status epilepticus |
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What are the uses of Phenytoin? Mechanism? |
- First line for tonic-clonic seizures |
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What are the side effects of Phenytoin? |
- Nystagmus |
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What form of Phenytoin can be taken for parenteral use? |
Fosphenytoin |
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What is Carbamazepine used for? Mechanism? |
First-line for: |
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What are the side effects of Carbamazepine? |
- Diplopia |
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What drug is first line for trigeminal neuralgia? |
Carbamazepine |
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What is Valproic Acid used for? |
- First-line for tonic-clonic seizures |
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What is the mechanism of Valproic Acid? |
- ↑ Na+ channel inactivation |
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What are the side effects of Valproic Acid? |
- GI distress |
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What is Gabapentin used for? Mechanism? |
Used for: |
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What are the side effects of Gabapentin? |
- Sedation |
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What is Phenobarbital used for? Mechanism? |
Used for: |
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What are the side effects of Phenobarbital? |
- Sedation |
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What is Topiramate used for? Mechanism? |
Used for: |
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What are the side effects of Topiramate? |
- Sedation |
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What is Lamotrigine used for? Mechanism? |
Used for: |
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What are the side effects of Lamotrigine? |
Stevens-Johnson Syndrome (must be titrated slowly) |
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What is Levetiracetam used for? Mechanism? |
Used for: |
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What is Tiagabine used for? Mechanism? |
Used for: |
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What is Vigabatrin used for? Mechanism? |
Used for: |
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What is Stevens-Johnson Syndrome? |
- Prodrome of malaise and fever followed by rapid onset of erythematous / purpuric macules (oral, ocular, genital) |
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Which epilepsy medications cause Stevens-Johnson Syndrome? |
- Ethosuximide |
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Which epilepsy medication causes gingival hyperplasia? |
Phenytoin |
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Which epilepsy medication causes hirsutism? |
Phenytoin |
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Which epilepsy medication causes SLE like syndrome? |
Phenytoin |
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Which epilepsy medication causes blood dyscrasias? |
Carbamazepine |
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Which epilepsy medication causes neural tube defects? |
Valproic acid |
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Which epilepsy medication causes kidney stones? |
Topiramate |
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Which epilepsy medication causes induction of cytochrome P-450? |
- Phenytoin |
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Which epilepsy medication is used for peripheral neuropathy? |
Gabapentin |
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Which epilepsy medication is used for post-herpetic neuralgia? |
Gabapentin |
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Which epilepsy medication is used for migraine prophylaxis? |
- Gabapentin |
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Which epilepsy medication is used for bipolar disorder? |
- Valproic acid |
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Which epilepsy medication is used first line for neonates? |
Phenobarbital |
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What are the types of barbiturates? |
- Phenobarbital |
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What is the mechanism of barbiturates? |
- Facilitate GABA-A actation by ↑ duration of Cl- channel opening |
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In what condition are barbiturates contraindicated? |
Porphyria |
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What are the clinical uses of barbiturates? |
- Sedative for anxiety |
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What are the possible side effects of barbiturates? |
- Respiratory and cardiovascular depression (can be fatal) |
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How do you treat an overdose of barbiturates? |
Supportive - assist respiration and maintain BP |
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What are the types of benzodiazepines? |
- Diazepam |
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What is the mechanism of benzodiazepines? |
- Facilitate GABA-A action by ↑ frequency of Cl- channel opening |
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Which benzodiazepines are short-acting? Implications? |
Higher addictive potential |
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Which benzodiazepines are longer-acting? Implications? |
Less addictive potential |
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What drugs bind the GABA-A receptor? |
Ligand-gated Cl- channel: |
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What are the clinical uses of benzodiazepines? |
- Anxiety |
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What are the side effects of benzodiazepines? |
- Dependence |
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How do you treat an overdose of benzodiazepines? |
Flumazenil (competitive antagonist at GABA benzodiazepine receptor) |
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What are the non-benzodiazepine hypnotics? |
All ZZZs put you to sleep: |
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What is the mechanism and clinical uses of non-benzodiazepine hypnotics? |
- Act via the BZ1 subtype of the GABA receptor |
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What are the side effects of non-benzodiazepine hypnotics? |
- Ataxia |
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What are the characteristics of CNS drugs? |
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? |
- Drugs with ↓ solubility in blood → rapid induction and recovery times |
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What is the MAC? |
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? |
Drugs with ↓ solubility in blood |
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What property makes an anesthetic have increased potency? |
Drugs with ↑ solubility in lipids |
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What are the types of inhaled anesthetics? |
- Halothane |
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What are the effects of inhaled anesthetics? |
- Myocardial depression |
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Which inhaled anesthetic causes hepatotoxicity? |
Halothane |
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Which inhaled anesthetic causes nephrotoxicity? |
Methoxyflurane |
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Which inhaled anesthetic causes proconvulsant effects? |
Enflurane |
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Which inhaled anesthetic causes expansion of trapped gas in a body cavity? |
Nitrous Oxide |
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What toxic side effect can all inhaled anesthetics cause? |
Malignant hyperthermia - 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 hyperthermia? |
Dantrolene |
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What are the types of IV anesthetics? |
- Barbiturates: Thiopental |
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Which IV anesthetic is high potency and high lipid solubility? Implications? |
Barbiturates (Thiopental) |
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What is Thiopental used for? |
- Induction of anesthesia |
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What terminates the action of Thiopental? |
Terminated by rapid redistribution into tissue (ie, skeletal muscle) and fat |
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What are the negative effects of Thiopental (IV anesthetic)? |
Decreases cerebral blood flow |
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What is the most common anesthetic used for endoscopy? |
Midazolam (benzodiazepine IV anesthetic) |
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What is Midazolam used for? |
- IV anesthetic used for endoscopy |
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What are the negative effects of Midazolam (IV anesthetic)? |
- Post-operative respiratory depression |
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What do you give a patient with overdose on IV Midazolam? |
Flumazenil |
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What type of IV anesthetic blocks NMDA receptors? |
Arylcyclohexylamines (Ketamine / PCP analog) |
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What is the mechanism of Ketamine? |
- PCP analog |
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What are the effects of Ketamine (IV anesthetic)? |
- Cardiovascular stimulant |
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What types of opioids can be used as IV anesthetics? |
- Morphine |
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What anesthetic can be used for sedation in the ICU? Mechanism? |
Propofol (IV anesthetic) - potentiates GABA-A |
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What are the characteristics of Propofol? |
- Rapid anesthesia induction |
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What are the types of local anesthetics? |
- Esters |
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What are the types of ester local anesthetics? |
- Procaine |
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What are the types of amide local anesthetics? |
Amides have 2 I's in name |
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What is the mechanism of local anesthetics? |
- Blocks Na+ channels by binding to specific receptors on inner portion of channel |
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How are tertiary amine local anesthetics different from other local anesthetics? |
Penetrate membrane in uncharged form, then bind to ion channels as charged form |
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How do you enhance the action of local anesthetics? |
Give with vasoconstrictors (usually epinephrine) to enhance local action. This decreases bleeding and increases anesthesia by decreasing systemic concentration. |
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What is the effect of alkaline anesthetics on infected (acidic) tissue? |
Alkaline anesthetics are charged and cannot penetrate membrane effectively. Thus, you need more anesthetic. |
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What is the order of nerve blockade when using local anesthetics? |
- small-diameter fibers > large diameter. |
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What is the order of loss when using local anesthetics? |
(1) pain, (2) temperature, (3) touch, (4) pressure. |
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What are local anesthetics used for? |
Minor surgical procedures, spinal anesthesia. |
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What should you give if patient is allergic to esters? |
Give amides. |
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What are the toxic side effects of local anesthetics? |
CNS excitation, severe cardiovascular toxicity (bupivacaine), hypertension, hypotension, and |
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What local anesthetic can cause severe cardiovascular toxicity? |
Bupivacaine |
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What local anesthetic can cause arrhythmias? |
Cocaine |
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What are neuromuscular blocking drugs used for? |
Used for muscle paralysis in surgery or mechanical ventilation. Selective for motor (vs. autonomic) nicotinic receptor. |
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What are the two types of neuromuscular blocking drugs? |
Depolarizing and Non-depolarizing |
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What is an example of a depolarizing blocking drug? |
Succinylcholine |
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What are the effects of Succinylcholine? |
Strong ACh receptor agonist; produces sustained depolarization and prevents muscle contraction |
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What are the phases of blockade? |
Phase I (prolonged depolarization) Phase II (repolarized but blocked; ACh receptors are available, but desensitized) |
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How do you reverse blockade of depolarizing blocking drugs in Phase I? |
Not possible. No antidote. Block potentiated by cholinesterase inhibitors. |
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How do you reverse blockade of depolarizing neuromuscular blocking drugs in Phase II? |
Antidote consists of cholinesterase inhibitors. |
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What are the complications of depolarizing neuromuscular blocking drugs? |
Complications include hypercalcemia, hyperkalemia, and malignant hyperthermia. |
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What are examples of nondepolarizing neuromuscular blocking drugs? |
- Tubocurarine |
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What is the mechanism of action of nondepolarizing neuromuscular blocking drugs? |
Competitive antagonists—compete with ACh for receptors. |
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What do you give to reverse blockade of nondepolarizing neuromuscular blocking drugs? |
- Neostigmine (must be given with atropine to prevent muscarinic effects such as bradycardia) |
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What is the mechanism of Dantrolene? |
Prevents the release of Ca2+ from the sarcoplasmic reticulum of skeletal muscle. |
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What are the uses of Dantrolene? |
Used to treat malignant hyperthermia and neuroleptic malignant syndrome (a toxicity of antipsychotic drugs). |
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What syndrome is a toxicity of antipsychotic drugs? |
Neuroleptic malignant syndrome |
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What is Parkinson disease caused by? |
Parkinsonism is due to loss of dopaminergic neurons and excess cholinergic activity. |
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What are the strategies to treat Parkinson disease? |
- Use Dopamine Agonists - Increase Dopamine - Prevent Dopamine Breakdown - Curb Excess Cholinergic Activity |
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What drugs are used as Dopamine agonists in the treatment of Parkinson disease? |
- Bromocriptine (ergot) - Pramipexole - Ropinirole (non-ergot)
Non-ergots are preferred |
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What drugs are used to directly stimulate Dopamine in the treatment of Parkinson disease? |
- Amantadine (may increase dopamine release) |
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What is a toxicity of Amantadine? |
Ataxia |
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What is Amantadine also used for? |
Used as an antiviral against influenza A and rubella. |
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What drugs are used to prevent Dopamine breakdown in the treatment of Parkinson disease? |
- Selegiline (selective MAO type B inhibitor) |
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What drugs are used to curb access cholinergic activity in the treatment of Parkinson disease? |
- Benztropine (Antimuscarinic; improves tremor and rigidity but has little effect on bradykinesia) |
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What is the mnemonic for drug treatment of Parkinson disease? |
BALSA: |
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What drugs do you use for essential or familial tremors? |
Use a beta-blocker (e.g., propranolol) |
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What is the mechanism of L-dopa (levodopa)? |
Increases level of dopamine in brain. Unlike dopamine, L-dopa can cross blood-brain barrier and is converted by dopa decarboxylase in the CNS to dopamine. |
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What is the mechanism of Carbidopa and why is it given with levodopa? |
Carbidopa is a peripheral decarboxylase inhibitor, is given with L-dopa to increase the bioavailability of L-dopa in the brain and to limit peripheral |
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What is L-dopa (levodopa) and Carbidopa used for? |
Parkinson Disease |
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What are the toxicities of L-dopa (levodopa) and Carbidopa? |
Arrhythmias from increased peripheral formation of catecholamines. Long-term use can lead to dyskinesia following administration (“on-off” phenomenon), akinesia between doses. |
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What is the mechanism of Selegiline? |
Selectively inhibits MAO-B, which preferentially metabolizes dopamine over norepinephrine and |
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What is Selegiline used for? |
Adjunctive agent to L-dopa in treatment of Parkinson disease. |
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What is the toxicity of Selegiline? |
May enhance adverse effects of L-dopa. |
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What drugs are used to treat Alzheimer? |
- Memantine (NDMA receptor antagonist) - Donepezil, galantamine, rivastigmine (AChE inhibitors) |
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What is the mechanism of Memantine? |
NMDA receptor antagonist; helps prevent excitotoxicity (mediated by Ca2+). |
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What are the toxicities of Memantine? |
Dizziness, confusion, hallucinations. |
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What is the mechanism of drugs such as Donepezil, galantamine, and rivastigmine? |
AChE inhibitors |
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What are the toxicities of Donepezil, galantamine, and rivastigmine? |
Nausea, dizziness, insomnia. |
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What are the neurotransmitter changes in Huntington disease? |
- Decreased GABA |
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What are the treatments for Huntington disease? |
- Tetrabenazine and reserpine - Haloperidol |
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What is the mechanism of Tetrabenazine and Resperine? |
Inhibit vesicular monoamine transporter (VMAT); limit dopamine vesicle packaging and release. |
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What is the mechanism of Haloperidol? |
Dopamine receptor antagonist |
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What is the mechanism of Sumatriptan? |
5-HT 1B/1D agonist. Inhibits trigeminal nerve |
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What are the uses of Sumatriptan? |
Acute migraine, cluster headache attacks |
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What are the toxicities of Sumatriptan? |
Coronary vasospasm, mild tingling. |
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Why is Sumatriptan contraindicated in CAD (Coronary Artery Disease) and Prinzmetal Angina? |
Causes Coronary Vasospasm |
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What is the mnemonic for Sumatriptan? |
A SUMo wrestler TRIPs ANd falls on your head. |