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154 Cards in this Set

  • Front
  • Back
Main Drug Classes Used to Rx Glaucoma?
Cholinomimetics
Beta Blockers
Which Cholinomimetics are high yield for Rx-ing Glaucoma?
Pilocarpine
Echothiopate
MOA of Pilocarpine for Glaucoma?
M-Receptor Agonist--->
contraction of ciliary muscle--->
INc flow through Canal of Schlemm
MOA for Echothiophate for glaucoma?
Organophosphate AChE Inhibitor-->
Inc Outflow
Which Beta-Blockers are used for Glaucoma?
Timolol
MOA for Timolol for Glaucoma?
Blocks NE's actions at Ciliary Epithelium--->
Dec production of Aqueous Humor
Rx for Closed Angle Glaucoma?
Surgery

Pre-Op:
Cholinomimetics
CA Inhibitors and/or Mannitol (dec body volume of water)
Drug class straight contraindicated in Closed Angle?
Antimuscarinics
Alpha 1 agonists
Who else can you use for Glaucoma (low yield)? kicker?
Epi: dec synthesis, SE = stinging; not for closed angle,
Brimonidine (alpha agonist)
Latanoprost (PGF-2alpha): inc outflow; SE: darkens iris
Difference between Pain Threshold and Tolerance?
Threshold is where you have the initial perception of pain
Tolerance is your Rxn to pain
Morphine's Fxns?
Analgesia: Inc pain tolerance (you feel it, you just don't care)
Sedation
Cough Suppression
SE's of Morphine?
Resp Depression (not good)
CV: minimal on heart, but vasodilates (avoid in head trauma)
GI: longitudinal's relax, circular constricts---> CONSTIPATION
MIOSIS***via E-W nucleus
N&V: stimulates CTZ in area postrema
Which is the only Opioid that doesn't cause MIOSIS? why?
Meperidine
it also blocks M receptors
#1 abused by health care professional
Which Opioid is the key for Cough Suppression?
DM
Dextromethorphan
Who are the Full Opioid Receptor Agonists?
Meperidine
Methadone
Fantanyl
Heroin
Key to Meperidine Metabolism?
Metabolized by P450---> Nomeperidine = SSRI that can cause Serotonin Syndrome (seizures)
Who are the Partial Opioid receptor agonists?
Codeine
Buprenorphine/Butorphanol
Kicker for Buprenorphine?
Acts as an antagonist in presence of Full agonists, which is Bad Bad for Substance Dependence b/c it precipitates withdrawal, so its contraindicated
Time Out: what are the Opioid receptors? who have we been talking about so far with morphine and all these other guys?
mu
kappa
delta

Mu is the guy we've been referring to. Mu is most pharmacologically important
Who are the Mixed Opioid Agonists?
Nalbuphine
Pentazocine
What other receptor do Nalbuphine and Pentazocine stimulate? result?
kappa: spinal analgesia and dysphoria
Issue w/ Nalbuphine and Pentazocine?
can precipitate withdrawal just like partial agonists
Who are the Opioid Receptor Antagonists/
Naloxone
Naltrexone
Pharm properties for Naloxone and Naltrexone?
Naloxone: short acting
Naltrexone: long duration, better bioavailability
uses for Naloxone?
IV
Reversal of Resp. Depression
Post-op reversal of fentanyl's effects
Uses and administration of Naltrexone?
PO
Dec craving for alcohol
Used after detox in opioid addicts
Mech for Naltrexone and booze?
Alcohol is addicting in part b/c of Enkephalins and Endorphins (endogenous opioids)
Naltrexone blocks these
What's up w/ Tolerance and opioids?
Occurs to all effects
EXCEPT
Miosis
Constipation (so as you raise dose to combat tolerance they get MORE CONSTIPATED)
Rx for Opioid Withdrawal?
FULL AGONIST (like methadone)
Who are the Opiate-related drugs w/ specific indications? why?
Loperamide: rx's diarrhea b/c it doesn't cross BBB
Dextromethorphan: Rx's Cough
Who is Tramadol? mech?
Very weak opioid agonist
Also inhibits 5-HT and NE reuptake
Use for Tramadol?
Chronic Pain
SE of Tramadol?
Dec seizure threshold
2 High Yield Mechanisms for Anticonvulsants? which drugs for each?
Dec axonal Conductions by Blocking Fast Na Channels
carbamazepine and phenytoin

Inc inhibitory tone by facilitating GABA-mediated hyperpolarization
barbs and benzo's
DOC for Partial Seizures (simple or complex?
Valproic Acid
Phenytoin
Carbamazepine
DOC for Tonic-Clonic (grand mal) Seizures (general)
Valproic Acid
Phenytoin
Carbamazepine
DOC for General Absence Seizures?
Ethosuximide
and Valproid Acid
DOC for Status epilepticus? ly
Benzo's (lorazepam, diazepam)
Phenytoin (fosphenytoin is better IV cause its water soluble)
MOA for Phenytoin?
blocks axonal Na channels in their Inactive state thus preventing seizure propagation
Pharmacokinetics for Phenytoin?
Induces cytochrome P450's
Zero-Order Elimination!!!
Who are the drugs eliminated via Zero-Order kinetics?
Phenytoin
Alcohol
Main SE for Phenytoin?
Gingival Hyperplasia!!!
What drugs cause Gingival Hyperplasia?
Phenytoin
Nifedipine
Cyclosporine
MOA for Carbamazepine?
same as phenytoin

blocks Na channels in inactive state
Other use for Carbamazepine?
DOC for Trigeminal Neuralgia
SE kickers for Carbamazepine? hy
Induces P450 (especially the ones that metabolize sex hormones---> dec efficacy of OCP's)

Inc ADH secretion---> SIADH and dilutional hyponatremia
Other drug that can cause SIADH?
Chlorpropramide (Sulfonylurea)
When talking about valproic acid, what do clinicians actually prescribe?
Divalproex Na
MOA of valproic acid? LY
similar to phenytoin
also inhibits GABA transaminase
blocks t-type Ca channels
Uses for Valproic Acid?
all Seizure types
Mania of Bipolar Disorders (soon to be DOC)
Migraine Prophylaxis (but not sx rx)
SE's of Valproic Acid?
Inhibits P450s
Hepatotoxic (from toxic metabolite)
Pancreatitis****
Teratogen--->Spina Bifida

Hepatotoxicity and pancreatitis can kill you
What other drugs can cause pancreatitis?
i don't know, but if there is a question about it, then Valproic Acid is the answer
MOA for ethosuximide?
LY
blocks t-type Ca channels and thalamic neurons
Uses for ethosuximide?
DOC for absence seizures
General SE for anticonvulsants?
Dec efficacy of OCP's via induction of P450's
New Anticonvulsants to know?
Felbamate
Lamotrigine
Uses for Felbamate and Lamotrigine
Broad spectrum
good for Seizure States
SE's for Felbamate and Lamotrigine
Felbamate:
hepatotoxic
Aplastic anemia (100% fatal)

Lamotrigine:
Stevens-Johnson Syndrome (40% develop rashes. 1% of those are S-J)
Why the heck is Felbamate and its hepatotoxicity and aplastic anemia still on the market?
Last line of defense
used for Lenox-Gusalt Syndrome
Gabapentin uses?
DOC for Neuropathic pain (except for trigeminal = carba...)
SE's of Ethosuximide?
Fatigue
GI
HA
What drugs can Cause SLE-like reactions?
Hydralazine
Isoniazid
Procainamide

quinidine
phenytoin
Benzo vs Barb toxicity?
Barbs have a much narrower therapeutic window before they kill you

So mostly we just use benzo's
MOA for Benzo's
Potentiate GABA
Inc frequency of Cl channel openings--->membrane hyperpolarization
Not GABA mimetic, so need GABA to be present
Act through BZ receptors on GABA complex
Different BZ receptors and their activity?
BZ1: sedation
BZ2: anti-anxiety and impaired cognitive fxn
Rx for Benzo and Barb OD?
Benzo: Flumazenil
Barbs: flumazenil doesn't work, you've just gotta Rx the sx's
MOA for Flumazenil?
Nonspecific BZ receptor antagonist--->reversal of CNS depression seen w/ OD or post-anesthesia
Examples of Benzo's?
Alprazolam
Diazepam
Lorazepam
Midazolam
Temazepam
Oxazepam
General Uses for Benzo's?
Anxiety
Panic attacks
Muscle relaxation
Withdrawal states (ethanol)
Status epilepticus (loraz and diaz)
Anesthesia amnesia (Midazolam)
Sleep Disorders (temaz and oxaz)
Rare uses of Barbs?
Phenobarbital: seizures
Thiopental: induce anesthesia
besides killing you (cns depression), what are SE's of barbs?
induce P450
Kickers for relationship between benzo's, barb's and booze?
Cross-tolerance to all 3
Barbs and booze are more likely to be abused
Withdrawal of any ---> life threating sx's (tonic-clonic status and DT's)
Rx for Barb or Ethanol
Long acting Benzo
(diazepam>lorazepam> the rest)
DDI's for Benzo's and Barbs?
additive w/ other CNS depressants

Induce P450 of most lipid-soluble drugs (like OCP's)
Who are the Non-Benzo's who act like Benzo's?
Zolpidem
Zaleplon
Buspirone
MOA for Zolpidem and Zaleplon?
BZ-1 receptor agonist
Uses of Zolpidem and Zaleplon?
Sleep disorders
MOA for Buspirone?
No effect on GABA
5-HT-1a partial agonist---> inc 5-HT activity
Use for Buspirone?
Generalized Anxiety Disorders (have low 5-HT)
Nonsedative
Downside to Buspirone?
takes 1-2 weeks to take effect

so no good for situational anxiety disorders
What is MAC?
Minimal Alveolar Concentration at which 50% of the population is anesthetized

Measure of potency: ED50
How does lipid solubility affect MAC?
The more Lipid Soluble the anesthetic, the Lower the MAC and the Greater the Potency

Inc Lipid Solubility = Dec MAC = Inc Potency
How does blood solubility affect MAC?
More Soluble in Blood = Slower Anesthetic onset
How do Blood:Gas Ratios affect Anesthetics?
High B:G ratio --> Slow onset
High B:G ratio---> Slow recovery
Low B:G ratio--->fast onset and recovery
Inhalational Anesthetics I need to know?
Nitrous Oxide
Halothane
MAC values for Nitrous and Halothane?
104% for Nitrous
0.8% for Halothane

so halothane is much more lipid soluble and much more potent
Blood:Gas Ratios for Nitrous and Halothane?
Nitrous: 0.5
Halothane: 2.3

So halothane is more blood soluble and thus has a slower onset
CV effects of Nitrous and Halothane? significance?
Nitrous: minimal

Halothane: sensitizes heart to Catecholamines (Beta 1's can lead to an arrhythmia. Ergo, don't ever put a pt w/ a pheochromocytoma under using halothane
SE's for Nitrous? how to prevent?
Diffusional Hypoxia

prevent w/ 100% O2 after use
SE's for Halothane?
Malignant Hyperthermia
Arrhythmias
Who are the IV Anesthetics?
Thiopental
Midazolam
Propofol
Fentanyl
Ketamine
Kickers for Thiopental?
Barb
Used for induction (not much anymore)
Highly lipid soluble
Rapid Onset
Short Acting due to redistribution?
what is redistribution?
Lipid soluble drug get redistributed to tissue (adipose) and thus decrease the duration of the drug
uses of Midazolam?
Anterograde Amnesia
Preop sedation
induction
Outpatient surgery

depresses resp
Use for Propofol?
INDUCTION and maintenance
ANTIEMETIC!!! (only anesthetic w/ this property)
CNS and cardiac depressant
Uses of Fentanyl?
Opiate for induction and maintenance
Depresses resp
MOA for ketamine?
Dissociative Anesthetic
NMDA Receptor Antagonist
Uses of Ketamine?
Induction

only used in kids cause they don't report...
SE's of Ketamine?
Emergent Delirium
Hallucinations (not in kids)
CV Stimulation
Inc ICP
Types of Local Anesthetics?
Esters and Amides
How do you tell the local anesthetics apart?
If it has just 1 "i" then its an ester

more than 1 "i" is an amide
So who are the local anesthetic esters and amides?
Esters: Procaine, Cocaine, Benzocaine

Amides: Lidocaine, Bupivacaine, Mepivacaine
How are Local Anesthetics metabolized?
Esters are metabolized by plasma and tissue esterases

Amides are metabolized by liver amidases
MOA for local anestetics?
The drug must cross the axonal membrane to fxn
In order to cross the membrane the drug must be in the non-ionized form.
In order to be active the drug must be in the ionized form.

The active, ionized drug blocks Fast Na channels in the inactive state

So there's a lot of stuff having to happen.
How do different nerve fiber differ in sensitivity to Local Anesthetics?
The smaller the diameter the more sensitive
AND
the higher the firing rate, the more sensitive
AND
myelinated are more sensitive than unmyelinated
based on the different factors affecting sensitivity what is the Order of Sensitivity for different nerve fibers? Significance?
Type B and C > A-delta > A-beta and A-gamma > A-alpha

This means we'll lose the nerves for pain (C's and A-deltas) way before we lose the nerve fibers for motor neurons (A-alphas)
How does recovery proceed?
in the reverse order of sensitivity. so motors first, pregang ANS fibers last
How are local anesthetics administered?
They're given w/ Alpha-1 agonists (vasoconstrictors) in order to stop the anesthetics from entering the systemic circ

Inc Duration and dec toxicity
SE's of Local Anesthetics?
Neurotoxic--->seizures
CV toxic (esp bupivacaine and cocaine)
Allergies: esters via PABA formation
Affect of pH on Local Anesthetics? clinical significance?
In acidic tissue, the drugs get stuck in the ionized (active) form and can't penetrate the axonal membrane

this occurs clinically in infections.

To fix just up the dose
Use of Neuromuscular blocking drugs? why they work?
Used for muscle paralysis in surgery or mech. ventilation.

Selective for motor (vs autonomic) nicotinic receptors
2 types of NM blocking drugs?
Nondepolarizing (competitive)
Depolarizing (noncompetitive)
MOA for Nondepolarizing NM blocking drugs?
Nicotinic Antagonists
Examples of Nondepolarizing NM blocking drugs?
D-Tubocurarine
Atracurium
Mivacurium

-cur- drugs
What do Nondepolarizing NM blocking drugs affect? not affect?
Paralysis of face, limbs, resp muslces

No effects on cardiac or smooth muscle

No CNS effects
1 reason to use Atracurium
and
1 reason not to use Atracurium?
It is safe in heptic and renal impairment

It is inactivated to Laudanosine, which can cause seizures
How to cause recovery from Nondepolarizing NM blocking drugs?
AChE Inhibitors (neostigmine)
MOA for Depolarizing NM blocking drugs? phases?
Nicotinic AGONIST

Phase 1 = depolarization, FASCICULATION, prolonged depol, flaccid paralysis

Phase 2: densensitization
Who are the Depolarizing NM blocking drugs?
How do you reverse them?
SUCCINYLCHOLINE!

you don't. AChE I's only make Phase 1 worse but will help Phase 2
Potential SE's of Depolarizing NM blocking drugs
MALIGNANT HYPERTHERMIA
hyperK
atypical pseudocholinesterase
Who are the Centrally Acting Skeletal Muscle Relaxants? MOA? use?
Benzo's
Baclofen

both work via GABA receptors

Used for spasticity
Rx for malignant hyperthermia?
Dantrolene
What causes malignant hyperthermia?
inhalation anesthetics (except nitrous)
Succinylcholine
MOA for Dantrolene?
prevents release of Ca from SR of skeletal muscle
Other uses of Dantrolene?
Neuroleptic Malignant Syndrome (toxicity of anti-psychotic drugs)
Drug types used to Rx Parkinson's?
DA receptor agonists
Inc DA
Prevent breakdown of DA
Block fxn of ACh
Primary Parkinson drug? MOA?
Levodopa
prodrug that gets converted by Aromatic AA decarboxylase to DA
How is Levodopa Administered? why?
With Carbidopa:
Carbidopa blocks AAAD and doesn't cross the BBB. This keep L-dopa from being converted to DA outside the CNS
SE's of Levodopa?
**Peak-dose dyskinesias
On-Off effects
**Psychosis (inc DA in mesolimbic)
Hypotension (makes post. instability worse)
Vomiting (activates CTZ)
Who else can help Levodopa?
Tolcapone (entacapone)
Selegiline
MOA for Tolcapone and Entacapone?
Inhibit COMT, which is good b/c COMT metabolizes DA

Inc uptake and efficacy
SE's of Tolcapone?
Hepatotoxic (not entacapone)
MOA for Selegiline?
MAO-b selective inhibitor
Why is it good the Selegiline is a selective MAO-b inhibitor?
b/c it means there isn't any wine/cheese HTN
Why is Selegiline almost always given w/ Levodopa?
It blocks the metabolism of DA in the CNS
SE's of Selegiline?
one of its metabolites is an amphetamine--->insomnia
Who are the DA receptor agonists for PD?
BROMOCRIPTINE
Pramipexole
ropinirole
PERGOLIDE
Other uses for Bromocriptine?
HyperPRL and Acromegaly since DA suppresses Prolactin and GH
Kicker for Pergolide?
off the market due to causing valvular defects
What drugs are used to Dec ACh fxn?
Benztropine*
Trihexyphenidyl
Diphenhydramine*
How do benztropine, diphenhydramine and trihexylphenidyl work?
They are Muscarinic blockers and thus block the effects of ACh--->Dec tremors and rigidity but have little effects on bradykinesia
SE's of the muscarinic blockers?
Anti-DUMBELLS
1 more drug that can be used for PD?
Amantidine
MOA for amantidine?
Anti-viral
Blocks M-receptors
Inc DA release
SE's of Amantidine?
Anti-dumbells
Livedo Reticularis
What is Livedo Reticularis?
Purple-ish lower legs
varicose veins to the max
Benign and reversile
Rx for essential or familial tremors?
beta blockers
MOA for Sumatriptan?
5-HT-1b/1d agonist
causes:
vasoconstriction
inhibition of trigeminal activation and vasoactive peptide release
Clinical Uses for Sumatriptan?
acute migraines (dec PAIN)
cluster HA's
2 big Alzheimer's Drugs?
Memantine
Donepezil
MOA for memantine?
NMDA receptor ANTAGONIST
helps prevent excitotoxicity
SE's of Memantine?
dizzy
confused
hallucinations
MOA for Donepezil?
AChE I
SE's of Donepezil?
Nausea
Dizzy
Insomnia