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Flashcards in Neuro Pharm from FA Deck (88)
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1

where are the M receptors on the eye? what is their function?

pupillary sphincter (M3)  - causes miosis

ciliary muscles (M3)  - accomodation

2

where are the a1 receptors on the eye? what is their function?

pupillary dilator (a1) 

causes mydriasis

3

where are the ß receptors on the eye? what is their function?

ciliary epithelium 

produces aqueous humor

4

Glaucoma Drugs: overall mechanism?

Decr IOP via decr amount of aqueous humor. (inhibit synthesis/secretion, or increase drainage)

5

Epinephrine.

Class? Mech? SE?

Class: Glaucoma drug, a1, ß1, ß2 agonist

Mech: decr aqueous humor synthesis via vasoconstriction via a1 receptors

SE: Mydriasis (pupil dilation); do not use in closed-angle glaucoma

6

Brimonidine

Class? Mech? SE?

Class: Glaucoma drug, Alpha-2 agonist

Mech: decr aqueous humor synthesis

SEs: Blurry vision, ocular hyperemia, foreign body sensation, ocular allergic reactions, ocular pruritis

7

Timolol, Betaxolol, Carteolol

Class? Mech? SE?

Class: Glaucoma drugs, beta-blockers

Mech: decr aqueous humor synthesis

SE: None given

8

Acetazolamide

Class? Mech? SE?

Class: Glaucoma drug, diuretic

Mech: decr aqueous humor synthesis via inhibition of carbonic anhydrase.

SE: None given

9

Pilocarpine, Carbachol

Class? Mech? SE?

Class: Glaucoma drugs, Direct cholinomimetics

Mech: incr outflow of aq humor via contraction of ciliary muscle and opening of trabecular meshwork

SE: Miosis and cyclospasm (contracton of ciliary muscle)

Note: use pilocarpine in emergencies - very effective at opening meshwork into canal of Schlemm

10

Physostigimine, Echothiophate

Class? Mech? SE?

Class: Glaucoma drugs, Indirect Cholinomimetic

Mech: incr outflow of aq humor via contraction of ciliary muscle and opening of trabecular meshwork

SE: Miosis and cyclospasm (contracton of ciliary muscle)

11

Latanoprost (PGF-2alpha)

Class? Mech? SE?

Class: Glaucoma drug, Prostaglandin

Mech: increased outflow of aqueous humor

SE: darkens color of iris (browning), and lengthens eyelashes (this was actually on the boards!!)

12

Big picture for glaucoma:

which drugs decr IOP by decreasing synthesis of aqueous humor? (6)

Alpha-agonists: Epinephrine, Brimonidine

Beta-blockers: Timolol, Betaxolol, Cartelol

Diuretics: Acetazolamide

13

Big picture for glaucoma:

which drugs decr IOP by increasing drainage/outflow of aqueous humor? (5)

Cholinomimetics: Pilocarpine, Carbachol, Physostigmine, Echothiophate

Prostaglandin: Latanoprost

14

List the opioid analgesics? (8)

Generally, clinical uses?

Morphine

Fentanyl

Codeine

Loperamide

Methadone

Meperidine

Dextromethorphan

Diphenoxylate

Clinical use of this class (every drug not used for every item): Pain control, cough suppression, diarrhea, acute pulm edema, maintenance programs for heroin addicts

15

Morphine

Class? Mech? Use? Toxicity?

Class: Opioid receptor agonist (mu receptor = morphine, delta = enkephalin, kappa = dynorphin). Modulates synaptic transmission -- opens K channels, closes Ca2+ channels -> decr synaptic transmission via hyperpolarization. Inhibits release of ACh, Norepi, 5-HT, glutamate, Substance P

Clinical use: Pain, Acute pulm edema

Tox: Addiction, resp depression, constipation, miosis, addictive CNS depression with other drugs. Tolerance does not develop to miosis and constipation. Tox treated with naloxone or naltrexone (opioid receptor antagonists)

16

Fentanyl

Class? Mech? Use? Tox?

Class: Opioid receptor agonist (mu receptor = morphine, ​delta = enkephalin, kappa = dynorphin). Modulates synaptic transmission -- opens K channels, closes Ca2+ channels -> decr synaptic transmission via hyperpolarization. Inhibits release of ACh, Norepi, 5-HT, glutamate, Substance P

Clinical use: Pain, Acute pulm edema

Tox: Addiction, resp depression, constipation, miosis, addictive CNS depression with other drugs. Tolerance does not develop to miosis and constipation. Tox treated with naloxone or naltrexone (opioid receptor antagonists)

17

Codeine

Class? Mech? Use? Tox?

Class: Opioid receptor agonist (mu receptor = morphine, ​delta = enkephalin, kappa = dynorphin). Modulates synaptic transmission -- opens K channels, closes Ca2+ channels -> decr synaptic transmission via hyperpolarization. Inhibits release of ACh, Norepi, 5-HT, glutamate, Substance P

Clinical use: Pain, Acute pulm edema

Tox: Addiction, resp depression, constipation, miosis, addictive CNS depression with other drugs. Tolerance does not develop to miosis and constipation. Tox treated with naloxone or naltrexone (opioid receptor antagonists)

18

Loperamide

Class? Mech? Use? Tox?

Class: Opioid receptor agonist (mu receptor = morphine, ​delta = enkephalin, kappa = dynorphin). Modulates synaptic transmission -- opens K channels, closes Ca2+ channels -> decr synaptic transmission via hyperpolarization. Inhibits release of ACh, Norepi, 5-HT, glutamate, Substance P

Clinical use: Pain, Acute pulm edema, Diarrhea

Tox: Addiction, resp depression, constipation, miosis, addictive CNS depression with other drugs. Tolerance does not develop to miosis and constipation. Tox treated with naloxone or naltrexone (opioid receptor antagonists)

19

Methadone

Class? Mech? Use? Tox?

Class: Opioid receptor agonist (mu receptor = morphine, ​delta = enkephalin, kappa = dynorphin). Modulates synaptic transmission -- opens K channels, closes Ca2+ channels -> decr synaptic transmission via hyperpolarization. Inhibits release of ACh, Norepi, 5-HT, glutamate, Substance P

Clinical use: Pain, Acute pulm edema, Maintenance programs for heroin addicts

Tox: Addiction, resp depression, constipation, miosis, addictive CNS depression with other drugs. Tolerance does not develop to miosis and constipation. Tox treated with naloxone or naltrexone (opioid receptor antagonists)

20

Meperidine

Class? Mech? Use? Tox?

Class: Opioid receptor agonist (mu receptor = morphine, ​delta = enkephalin, kappa = dynorphin). Modulates synaptic transmission -- opens K channels, closes Ca2+ channels -> decr synaptic transmission via hyperpolarization. Inhibits release of ACh, Norepi, 5-HT, glutamate, Substance P

Clinical use: Pain, Acute pulm edema

Tox: Addiction, resp depression, constipation, miosis, addictive CNS depression with other drugs. Tolerance does not develop to miosis and constipation. Tox treated with naloxone or naltrexone (opioid receptor antagonists)

21

Dextromethorphan

Class? Mech? Use? Tox?

Class: Opioid receptor agonist (mu receptor = morphine, ​delta = enkephalin, kappa = dynorphin). Modulates synaptic transmission -- opens K channels, closes Ca2+ channels -> decr synaptic transmission via hyperpolarization. Inhibits release of ACh, Norepi, 5-HT, glutamate, Substance P

Clinical use: Pain, Acute pulm edema, Cough suppression

Tox: Addiction, resp depression, constipation, miosis, addictive CNS depression with other drugs. Tolerance does not develop to miosis and constipation. Tox treated with naloxone or naltrexone (opioid receptor antagonists)

22

Diphenoxylate

Class? Mech? Use? Tox?

Class: Opioid receptor agonist (mu receptor = morphine, ​delta = enkephalin, kappa = dynorphin). Modulates synaptic transmission -- opens K channels, closes Ca2+ channels -> decr synaptic transmission via hyperpolarization. Inhibits release of ACh, Norepi, 5-HT, glutamate, Substance P

Clinical use: Pain, Acute pulm edema, Diarrhea

Tox: Addiction, resp depression, constipation, miosis, addictive CNS depression with other drugs. Tolerance does not develop to miosis and constipation. Tox treated with naloxone or naltrexone (opioid receptor antagonists)

23

Butorphanol

Class? Mech? Use? Tox?

Class: Opioid agonist

Mech: Mu-opioid receptor partial agonist and kappa opioid receptor agonist. Causes analgesia

Use: Severe pain (labor, migraine). Causes less resp depression than full opioid agonists

Tox: If pt is also taking full opioid agonist, can cause opioid withdrawal symptoms (due to competition for opioid receptors). Overdose not easily reversed with naloxone

24

Tramadol

Class? Mech? Use? Tox?

Class: Opioid agonist (weak)

Mech: Very weak opioid agonist. Also inhibits serotonin and norepi reuptake - works on multiple neurotransmitters ("tram it all" in with tramadol)

Use: Chronic pain

Tox: similar to opioids. Decreases seizure threshold. Serotonin syndrome.

25

Epilepsy: First line drug for Simple Partial seizure?

Carbamazepine

26

Epilepsy: First line drug for Complex Partial seizure?

Carbamazepine

27

Epilepsy: First line drugs for Generalized Tonic-Clonic seizure? (3)

Phenytoin, Carbamazepine, Valproic acid

28

Epilepsy: First line drug for Absence seizure?

Ethosuximide

(Sucks to have Silent Seizures)

29

Epilepsy: First line drug for Status Epilepticus (Acute)?

Benzodiazepines (diazepam, lorazepam)

30

Epilepsy: First line drug for prophylaxis of Status Epilepticus?

Phenytoin