Drugs of Block IV

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ASA (acetylsalicylic acid) 1. Class 2. Indications 3. MOA 4. Adverse effects: 1. NSAID, analgesic,
2. low intensity, non-visceral pain, decrease inflammation
3. Irreversible COX inhibitor which inhibits production of thromboxanes and prostaglandins
4. toxicity easy to achieve. Symptoms = tinnitus, metabolic acidosis, incr. thirst.
Acetaminophen (Tylenol) 1. Class 2. Indications 3. MOA 4. Adverse effects/other: 1. Non-opioid analgesic with no antinflammatory actions
2. headache, any CNS pain
3. Binds COX in CNS (DOES NOT BIND TO COX IN PNS), less effective than NSAIDs.
4. toxicity at high doses
Often combined with ASA or caffiene: this antagonizes analgesic action
Ibuprofen 1. Class 2. Indications 3. MOA 4. Adverse effects/other: 1. NSAID, analgesic, antipyretic, anti-infl.
2. pain, inflammation, fever
3. Reversible COX inhibitor
4. Usually sold in racemate form: naproxen sold in active form only.
Sundilac 1. Class 2. Indications 3. MOA: 1. Prodrug - inactive. Active form - analgesic, antipyretic, anti-inflam.
2. Pain, fever, inflammation
3. Active drug is sulfide metabolite: this form is a reversible COX inhibitor and mediates analgesic, antipyretic and anti-infl. actions
Ketorolac 1. Class note to remember: 1. analgesic
note to remember - can be given in parenteral form for people who can't swallow, used in ER for suspected opioid receptors
Cox II inhibitors 1. enzyme they are selective for? 2. problems?: 1. inhibits enzyme responsible for prostaglandin synthesis
2. No better than NSAIDs and have more complications (ie. cardiovascular ones)
1. Why is morphine not as potent when given orally? 2. What is an opioid that is potent absorbed orally?: 1. potency is reduced by first pass metabolism in liver.
2. Codeine (oral administration is preferred)
People with a _________ deficiency cannot metabolize codeine.: CYP2D6
How and where are opioids metabolized?: in the liver
glucuronidation -> glucuronide is excreted in urine and bile
Why does heroin produce an analgesic effect?: It is metabolized to morphine INSIDE THE CNS. Normally morphine crossess the blood-brain-barrier less easily (heroin and codeine cross the BBB easily)
Once pain is relieved, how do you adjust the morphine dose?: Decrease it (less morphine is needed to prevent the recurrence of pain than to relieve it)
What is the ideal way to administer morphine to maximize the analgesic effect?: Give every 4 hrs. around the clock, NOT PRN. If pain breaks through: increase dose, not schedule.
Levorphanol 1. Class 2. Indications 4. Adverse effects/other: 1. opioid class (similar to morphine but metabolized more slowly)
2. used pre-op to potentiate and prolong general anesthesia
4. Respiratory depression and strong sedation common (although less vomiting and nausea than morphine)
Meperidine (Demerol) 1. Class 2. Adverse effects/other: 1. opioid (similar to morphine but weaker)
2. given parenterally, Adverse effects are tremors, dizziness, uncoordinated mvmnts, other CNS excitation signs.
DO NOT mix with barbituates - will cause unmaneagable CNS excitation
Fentanyl, Sufentanyl, Alfentanyl 1. Class 2. Indications 3. Adverse effects/other: 1. opioid - VERY POTENT (100x stronger than morphine)
2. used during surgery, pre- and post - op
3. immediate onset after IV, minimal CV effects, respiratory depression
Methadone 1. Class 2. Indications/Notes: 1. oral opioid analgesic
2. Similar to morphine but has longer duration and less sedation.
Can suppress heroin/morphine withdrawal symptoms (DRUG used to treat heroin addicts)
Propoxyphene (Darvon) 1. class/indications 2. Adverse effects/notes: 1. similar to methadone but weaker
2. restlessness, tremor, mild euphoria, convulsions. Potentiates ALCOHOL and tranquilizers - causes many drug-related deaths
Naloxone/Naltrexone 1. MOA 2. Indications: 1. competitive antagonist of opioids, acts at mu receptors
2. administer to reverse opioid overdose. Will block analgesia, reduces opioid effects within 1 minute
Pentazocine (Talwin): opioid, used to treat chronic and severe pain because of its sedative effects.
Butorphanol: potent analgesic(5x morphine)
barbituate like effect reduces abuse potential
Dextromethorphan, Codeine, Levopropoxyphene are all ________________.: antitussive drugs.
opioids: antitussive actions observed at lower doses than needed for analgesia. anitussive effects mediated at central and peripheral sites
Tubocurarine, Pancuronium 1. Class 2. Indications 3. MOA: 1. non-depolarizing neuromuscular blockers
2. used along w/ general anesthesia to cause flaccid paralysis (ie. abd. surgery)
3. neuromuscular blocker
MOA of neuromuscular blockers 1. non-depolarizing 2. depolarizing: 1. competitive antagonist at nicotinic receptors: causes flaccid paralysis
2. agonists at nicotinic receptors: resist degradation by AChE: sustained depolarization: muscle twitching prior to paralysis
Decamethonium,Succinylcholine Class Which one long acting? Why?: polarizing neuromuscular blockers
decamethonium - long acting (not hydrolyzed by AChE)
succinulcholine - short acting (hydrolyzed by AChE)
Ganglionic Blockers MOA (3) Use?: 1. Inhibition of vesicular release of ACh
2. Depolarizing blockers, resistant to AChE degradation
3. Nicotinic Receptor Agonists
*use is highly limited: control of BP during aortic surgery
Name a ganglionic blocker: trimethaphan
Cholinergics (aka. anticholinesterases, indirect cholinergic agonists) 1. MOA 2. Name 1 long and 1 short acting: 1. AChE inhibitors
2. Short acting - Edrophonium (Tensilon)
Long Acting - Neostigmine
What's the deal with irreversible cholinergics?: Usually toxins
Sarin, insecticides
Cholinomimetics 1. MOA: 1. muscarinic receptor agonists (mimic ACh), resistant to AChE
Bethanecol 1. Class 2. Tx.: 1. cholinomimetics
2. tx. of post-op or post-partum urinary retention (causes bladder contraction)
Pilocarpine 1. Class 2. Tx 3. Adverse effects: 1. Cholinomimetic
2. tx. for glaucoma, also topically used for induction of miosis in opthalmic exam
3. ciliary spasm
Anticholinergics MOA: muscarinic receptor agonists
Atropine 1. Class 2. Tx/Notes: 1. Anticholinergic
2. causes mydriasis and paralysis of accomodation in opthalmic exam; also reduction of respiratory secretions, prevention of bradycardia
Scopolamine 1. Class 2. Tx: 1. Anticholinergic
2. motion sickness, post-op nausea and vomiting
1. Ipratropium - class, tx. 2. Tolterodine - class, tx: 1. anticholinergic;
Tx - bronchospasm
2. anticholinergic;
Tx - overactive bladder
Amphetamine 1. Class 2. Tx 3. MOA: 1. Indirect sympathomimetic
2. psychomotor stimulant
3. taken up into presynaptic terminal, causes increased release of NE from same terminal.
Ephedrine 1. Class 2. Tx 3. MOA: 1. Direct sympathomimetic
2. psychomotor stimulant
3. analog of NE and E; can bind to receptors and have sympathetic effects
Methylphenidate 1. class 2. Tx.: 1. psychomotor stimulant
2. Tx. ADHD
Dextroamphetamine 1. class 2. Tx.: 1. psychomotor stimulant, analeptic
2. Tx: narcolepsy
Desipramine, Amyitriptyline 1. class 2. Tx. 3. MOA: 1. TCA
2. depression
3. Block reuptake of NE (If SSRI - blocks seratonin via 5-HT). This leaves more NE (or seratonin) in the synaptic cleft.
Phenylzine 1. Class 2. Tx. 3. MOA/Adverse Effects: 1. MAO inhibitors (specifically MAO-A)
2. depression
3. Blocks degradation of NE. orthostatic hypotension
Selegiline 1. Class 2. Tx 3. MOA: 1. MAO inhibitor (specifically MAO-B)
2. Parkinson's disease
3. Block degradation of NE, leaving more NE to act in the synaptic cleft
Nafcillin 1. Class 2. Indications 3. MOA 4. Notes/adverse reactions: 1. Antibiotic
2. Infection (mostly staph)
3. Inhibits cell wall synthesis (stops crosslinking) -> bacteriocidal
Pyridostigmine (Mestinon) 1. Class 2. Indications 3. MOA 4. Notes/adverse reactions: 1. Anticholinesterase
2. Myasthenia Gravis
3. inhibits acetylcholinesterase, ultimately allowing Ach to stay in NMJ longer.
4. must take dose on time
Azothioprine (Imuran) 1. Class 2. Indications 3. MOA 4. Notes/adverse reactions: 1. Immunosuppressant
2. autoimmune disorders (Crohn's, MG, Lupus etc)
3. Decreases purine metabolism thereby inhibiting DNA/RNA synthesis.
Carbamezepine 1. Class 2. Indications 3. MOA 4. Notes/adverse reactions: 1. anti-epileptic
2. seizures, tic-delaroux, manic depression
3. blocks Na+ channels; this decreases AP propagation leading to decreased seizure activity.
4. Interacts with CYP drugs.
Amitryptyline 1. Class 2. Indications 3. MOA 4. Notes/adverse reactions: 1. TCA
2. depression
3. seratonin and NE reuptake inhibitor (inhibits membrane pump)
4. interacts with drugs metabolized by P450
Propoxyphene 1. Class 2. Indications 3. MOA 4. Notes/adverse reactions: 1. Narcotic analgesic
2. Pain
3. binds to mu-opioid receptor
Buspirone Hydrochloride 1. Class 2. Indications 3. MOA 4. Notes/adverse reactions: 1. Anxiolytic
2. generalized anxiety disorder
3. Using the seratonin 5-HT receptor: increases K+ conductance and hyperpolarizes neuron.
Alprazolam (Xanax) 1. Class 2. Indications 3. MOA 4. Notes/adverse reactions: 1. Anxiolytics, benzodiazepenes
2. generalized anxiety disorder, panic disorder
3. binds to GABA receptors and enhances GABA effects.
Sertraline Hydrochloride (Zoloft) 1. Class 2. Indications 3. MOA 4. Notes/adverse reactions: 1. SSRI, antidepressant
2. depression, panic disorder
3. Inhibition of seratonin uptake at the 5-HT receptors
Gabapentine 1. Class 2. Indications 3. MOA 4. Notes/adverse reactions: 1. Anticonvulsant
2. partical seizures
3. Designed as a GABA analog - binds to Ca++ channels affecting polarity of neuronal membrane
Tramadol Hydrochloride 1. Class 2. Indications 3. MOA 4. Notes/adverse reactions: 1. Narcotic - like analgesic
2. pain
3. synthetic codeine analog. weak mu-receptor agonist, inhibits seratonin, NE uptake.
Rituxumab 1. Class 2. Indications 3. MOA 4. Notes/adverse reactions: 1. Monoclonal antibody
2. immune diseases
3. binds to CD20 receptor on surface of B-cell, mediates lysis from inside. Cytotoxic
4. many side effects - essentoally chemotherapy
Baclofen 1. Class 2. Indications 3. MOA 4. Notes/adverse reactions: 1. skeletal muscle relaxant
2. MS, muscle spasms, neuropathic pain
3. GABA analog, blocks afferent pathways in the spinal cord - result is decreased excitatory input to alpha motor neurons
Interferon Beta-1a 1. Class 2. Indications 3. MOA 4. Notes/adverse reactions: 1. immunomodulator
2. MS, Hep C
3. Decreases INF-gamma production. Decreases CD8 T-cells, myelin degradation and autoimmune reactions. Also inhibits T-helper cells.
Mycophenolate (CellCept) 1. Class 2. Indications 3. MOA 4. Notes/adverse reactions: 1. immunosuppressant
2. any autoimmune disease
3. inhibits lymphocyte DNA synthesis by inhibiting (IMPDH) enzyme that converts IMP to GMP. GMP needed for DNA synthesis.
Heparin 1. Class 2. Indications 3. MOA 4. Notes/adverse reactions: 1. anticoagulant
2. prophylaxis and treatment of thromboemobolitic disorders
3. causes conformational change in antithrombin-3, thus increasing the rate of thrombin inactivation by AT-3. Also prevents conversion of fibrinogen to fibrin
4. use with caution in hemorrhage or other bleeding disorders.
Warfarin (Coumadin) 1. Class 2. Indications 3. MOA 4. Notes/adverse reactions: 1. anticoagulant
2. prophylaxis and treatment of thromboembolitic disorders
3. Inactivates clotting factors. Does this by inhibiting vitamin K reductase = no vitamin K = no activation of clotting factors.
4. use with caution in hemorrhage or other bleeding disorders
Enalapril Maleate (Vasotec) 1. Class 2. Indications 3. MOA 4. Notes/adverse reactions: 1. ACE inhibitor
2. HTN, CHF
3. inhibits ACE: this blocks negative feeback to RAAS system allowing it to continue.
Pramipexole (Mirapex) 1. Class 2. Indications 3. MOA 4. Notes/adverse reactions: 1. antiparkinsonian agent
2. parkinson's disease
3. Dopamine Agonist - binds to D2 and D3 receptors in substantia nigra
4. watch for orthostatic hypotension.
Prazosin 1. Class 2. Indications 3. MOA 4. Notes/adverse reactions: 1. Alpha 1 blocker
2. HTN
3. binds to alpha one receptors and blocks them: result is decreased vascular resistance and decreased venous return.
4. watch for orthostatic hpotension
Seligilene 1. Class 2. Indications 3. MOA 4. Notes/adverse reactions: 1. antiparkinsonian agent, dopaminergic
2. PD
3. Irreverible inhibition of MAO-B receptor. This decreases dopamine breakdown in the corpus striatum; neuroprotective by preventing formation of free radicals
4. administer with Carbidopa/Levodopa
Clopidogrel Bisulfate (Plavix) 1. Class 2. Indications 3. MOA 4. Notes/adverse reactions: 1. antiplatelet
2. prevention of stroke, MI
3. inhibits platelet aggression via direct inhibition of ADP binding to it's receptor. Without ADP the activation of the glycoprotein complex cannot occur: so platelets don't aggregate
4. use with caution in pts. that have bleeding risk
Atorvastatin Calcium (Lipitor) 1. Class 2. Indications 3. MOA 4. Notes/adverse reactions: 1. Statin
2. slows the production of cholesterol to help prevent heart diesease, strokes etc.
3. inhibitor of HMG-CoA reductase - an important enzyme in cholesterol biosynthesis.
Gentamicin 1. Class 2. Indications 3. MOA 4. Notes/adverse reactions: 1. aminoglycoside antibiotic
2. serious infection
3. interferes with protein synthesis by causing misreading and premature termination of translation of mRNA. Bactericidal
Doxazocin mesylate (Cardura) 1. Class 2. Indications 3. MOA: 1. alpha 1 adrinergic antagonist
2. HTN, benign prostatic hyperplasia
3. for BPH: decreases smooth muscle tone of prostate bladder: decreases urethral resistance. for HTN: blocks alpha 1 receptors resulting in a decrease of vascular resistance.

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