Pharmacology Study guide #3:

The test three study guide if finally here! I have the drugs arranged into the categories of indication, slightly alphabetized, and the drugs and categories are all bold. This is a very long list of these drugs and if there is anything that you would like to add or change please leave a comment and I will make the adjustment as soon as possible.

Quick tip! If you are looking for a specific drug, search the text using “Command + F” on mac, and on pc open the edit drop down and click find on this page, maybe.

Happy studying!

-Peter

Anesthesia and analgesia

  • Acetaminophen (Tylenol)
  • anti-prostaglandin
  • metabolized in liver (watch out for this)
  • 3 g per day is the most dose per day
  • works in CNS
  • low GI irritation
  • can be used with kids
  • s/e: liver damage with ETOH is a high risk,
  • toxicity: 25 grams for adult
    • top cause of acute liver failure
    • the OD patient will die in 3-5 days from the liver damage
  • Acetylsalicylic acid Aspirin (ASA) – COX 1
      • gen 1 NSAID
      • inhibits platelet aggregation until there is a reproduction of more platelets
        • irreversible in the platelets that it affects
      • anti prostaglandin (inflammation)
      • do not use in kiddos
      • s/e: salicylism (ringing in ears points towards OD), reye’s syndrome, Renal impairment
      • Too Much? Tinnitus, respiratory depression, HypERthermia, can cause metabolic acidosis, then resp alkalosis to compensate.
  • COX inhibitors
    • COX 1: promotes Platelet aggregation, GI protection, renal fxn, (GOOD)
    • COX 2: promote inflammation (bad)
  • Anticholinergics
      • Can be used in pre anesthesia to reduce secretions
  • “Caine” drugs for numbing
      • local anesthesia
      • for: fingers, ears, nose, toes, and those
  • Codeine
  • Narcotic
  • *1/10th power of morphine
  • 5x power of aspirin, or acetaminophen
  • Epinephrine with Lidocaine
      • keeps the lidocaine local due to the vasoconstrictive properties of epi
  • Celecoxib (Celebrex) – COX 2
      • similar strength to ibuprofen
      • less stomach ulcers than other NSAIDs (some evidence)
  • Fentanyl
  • narcotic
  • **one hundred times stronger than morphine
  • Lollipop form in some cases for chronic pain (cancer)
  • will kill a kiddo!
  • -fluranes
      • Isoflurane
      • Strong anesthetic
        • weak analgesic
      • Volatile liquids mixes with O2 and inhaled
      • Resp depression, HYPOtension, arrhythmias, Hyperthermia
      • ***can be mixed with Nitrous oxide
        • for the strong analgesic properties
        • allows for a lower amount of each inhalant to get the desired effect, which lowers the risk for depression of resp. and the heart
  • Ibuprofen (Motrin, Advil) – COX 1
      • S/E: can cause renal damage, and GI bleeding, Retention of NA and H2O (watch out for HF patients)
  • Inhaled anesthetic agents
      • Works very quickly
  • IV anesthesia agents
      • lasts longer than inhaled
  • Methadone
  • narcotic
  • longest duration of action
  • long QT interval
  • for coming off of narcotics and given in clinics
  • Meperidine (Demerol)
  • narcotic
  • same action as morphine with a shorter action
  • treats post anesthesia shivers or rigors that can occur
  • no cough suppression effect
  • Morphine
  • narcotic
  • moderate to severe pain
  • can be given through almost all routes
  • cross BBB
  • S/E: resp depression, constipation, nausea, Miosis(pinpoint pupils)
  • morpheus god of sleep
  • give before the pain occurs if possible
  • PCA pump allows for the patient to not fall out of the TPR
  • is better than PRN, or fixed schedule
  • decreases overdose
  • can use smaller doses
  • empowers patient
  • cross olerance to other opiates
  • Naloxone (Narcan)
      • opiate antidote
      • also given when there is an OD of unknown cause
  • NSAIDS
      • gen 1: inhibit COX one and two
        • inhibit inflammation
        • inhibits prostaglandins in the stomach, so there is a higher chance for ulcers
      • Gen 2:
      • some studies show slowed healing of muscle, bone and ligament injuries.
  • Propofol
      • rapid onset and short duration
      • no analgesic effect
      • s/e: resp depression, rhabdo
  • Tramadol (Ultram)
      • Non opiate CNS acting analgesic
      • schedule 4
      • not an opiate but binds to the receptor
  • Pyridium (Phenazopyridine)
    • Treats pain from lower UTI’s
    • do not take if the pt has DM, or liver Dx
    • can cause a bright red or orange urine,take with food or there may be a Headache after dose
    • OTC

HA and migraines

All of these drugs vasoconstrict except for CCB and beta blockers. OTC is the most effective, and Ergot is not prescribed often

  • Beta-blockers and Calcium Channel Blockers
    • are prophylactic and chronically reduce the BP and cause the vessels to be less spastic.
  • Ergot Alkaloid
  • Ergotamine
      • for prophylaxis of migraines,
      • Alpha blocker vasoCONstriction
      • Rebound HA
      • S/E: HTN, MI trigger
      • increased risk of stillborn pregnancy increased uterine stim, and decreases the blood flow to the placenta
      • separate 24hrs between the use of ergotamine and sumatriptan.
      • related to ACID
  • Excedrin Migraine
    • OTC
    • one of the best if not the best remedy for HA and migraines
    • formulation: ASA, ibuprofen, and some caffeine
    • basic and effective
  • Triptans
    • Serotonergic  
    • sumatriptan and zolmitriptan
    • stim 5 – HT in the brain
    • it vasoconstricts and inhibits inflammation
    • not for prophylaxis of migraines only treat
    • S/E: stroke, MI, cerebral hemorrhage
    • WAIT 2 weeks to use a MAO-I med
    • DON’T take within 24 hours of ergotamine
      • toxicity w/ other 5-ht blockers, prozac,paxil, zoloft

Parkinson’s

too much ACH and not enough DA causing dyskinesia and Akinesia. Drugs do not cure but only slow the decline of symptoms, and treat the Bradykinesia, Gait, and improve daily activities. Comes from the degeneration in the extrapyramidal system which controls posture and gait (and others)

  • Anticholinergic
      • reduce ACH to bring balance to the Dopamine/ACH teeter totter
      • Benzotropine (Cogentin) and trihexyphenidyl (Artane)
          • similar to atropine, antimuscarinic
  • Dopaminergic
      • MAO-B inhibitors are used in patients with mild symptoms
  • Selegiline and rasagiline
          • inhibit DA breakdown
        • when the symptoms are increased, given meds change to levodopa and Dopamine agonist
        • S/E: drooling, constipation
  • Levodopa
        • DA prodrug
        • best effect in the first two years
        • take time off the drug “holiday”
        • many d/d interactions
        • vitamin B6 allows less levodopa to get to the CNS
  • Carbidopa
          • no bad effects on its own
          • increase usable levels of levodopa in the CNS
            • Is the CAR that drives levodopa to the CNS
  • COMT inhibitors:
  • blocks breakdown of Levodopa
  • Entacapone, and Tolcapone
        • CAPONE “protects” levodopa, like the mob
  • Levodopa/Carbidopa (Sinemet)
  • Levodopa/Carbidopa/Entacapone (Stalevo)
  • increase TP effects by stopping the breakdown of Levodopa
  • more convenient than taking 3 pills
  • Pramipexole (Mirapex)
  • dopamine agonist
  • first given alone in early parkinson’s then added to Levodopa in late.
  • S/E: sexy grandpa/grandma
  • MAO Inhibitors
    • 2 kinds
      • MAOA helps metabolize norepinephrine and serotonin
      • MAOB metabolizes dopamine
        • Selegiline (Eldepryl) inhibits this so DA is not metabolized.
      • food interactions: aged cheeses and meats, yeast, bread, BEER
      • stop antidepressants 2-7 weeks befor using
  • Selegiline
    • MAOI
    • look MAOI’s
    • many s/e and dd interactions
  • Tricyclic antidepressants (Amitriptyline)
  • Are the only antidepressants that should be used in PA
  • Do not use is ALZ
  • blocks ACH

Alzheimers

progression can only be slowed not cured. Medicine is creating new treatments, and there is a link to chromosome 21 (like in down’s). Tangles in the brain may be related to cholesterol so statins may be useful for prophylaxis. Know the lifestyle risk factors: low activity and education, smoking, DM, HTN, depression.

  • Memantine (Namenda) NMDA antagonist
  • Regulates calcium influx into the neuron
  • Indication is moderate to severe AD, but some neurologists start it early with Aricept
  • SE: dizzy, HA, confusion, constipation, hallucination
  • donepezil (Aricept) Acetylcholinesterase inhibitors
  • stop ACHesterase, increasing ACH
  • treatment of early dementia

Antimicrobials

  • Antivirals
  • Acyclovir (Zocirax)
      • similar to a purine nucleoside, and suppresses protein synthesis
      • S/E: phlebitis, nephrotoxic, stinging sensations.
  • Flu drugs:
      • Amantadine
  • Oseltamivir (Tamiflu)
    • Interferon alpha-2b
      • For hep B
      • causes flu like symptoms, and Hep causes flu like symptoms….
    • Ribavirin
      • Treats hep C with pegylated interferon-Alpha and a PI
  • HIV drugs
      • Reverse transcriptase, protease, and integrase are main targets of treatment to disrupt the virus.
      • HAART therapy – highly active antiretroviral therapy. two nucleoside reverse transcriptase inhibitors, and a protease inhibitor.
      • six classes of drugs to treat HIV
        • Non-nucleoside reverse transcriptase inhibitors (NNRTIs) Nucleoside reverse transcriptase inhibitors (NRTIs) Protease inhibitors (PIs) Fusion inhibitors, CCR5 antagonists or entry inhibitors (CCR5s) Integrase strand transfer inhibitors (INSTIs)
        • focus on the first three plus the fusion inhibitors
          • examples
            • NRTI: Zidovudine (Retrovir)
              • stops replication, slows the Dx, and increases the white blood cell (CD4) levels
              • Two of these are in the First set of Meds given along with on of the following: INSTI, NNRTI, or PI
            • NNRTI: Nevirapine (Viramune) Efavirenz (sustiva)
              • binds reverse transcriptase and stops the transcription
              • Can be a part of the first line of meds along with two NRTI’s
            • PI: Indinavir (Crixivan)
              • very effective
              • Can be a part of the first line of meds along with two NRTI’s
            • FI: Fuzeon, T-20
              • fusion inhibitors
              • stops HIV envelope from fusing with a CD4 cell membrane.
            • INSTI (HIV)- Integrase strand transfer inhibitors
              • Can be a part of the first line of meds along with two NRTI’s
  • CCR5 Antagonist (HIV) – Maraviroc (selzentry)
            • Entry inhibitors
            • Blocks HIV from binding to the CD4 cell (similar to the FI)
            • Can have an allergic rxn, cough, nausea, dizzy
  • Antibiotics
  • Aminoglycosides
        • Inhibit protein synthesis and are bactericidal
        • Causes injury to the inner ear and Kidneys
          • Nephro, and Ototoxic that is permanent
        • Narrow spectrum
        • draw drug levels
          • Peak thirty minutes after IV
          • Trough an hour before the next dose
          • given once a day
  • Amoxicillin
        • Broad spectrum
        • Aminopenicillins
        • disrupt cell wall with beta lactam ring
        • Amoxicillin and Clavulanic acid is Augmentin
          • This increases the effectiveness by breaking down the PenASE enzyme
  • Antibiotic resistance
  • Bacteria can adapt to a drug and create defences from a drug such as the PenicillinASE enzyme.
    • Carbapenems:
  • Imipenem (primaxin)
    • broad spectrum
    • resistant to beta lactam break down (penASE resistant)
    • used in Pseudomonas aeruginosa
    • Superinfections are an adverse effect as well and an allergic RXN
    • Cephalosporins
      • break down cell wall, for G+ and an increasing effectiveness with G-
      • bactericidal, and more resistant to PenASE than penicillin
      • spectrum broadens from gen 1 and 2 (narrow) to gen 3 and 4 are broad
      • ADME: poorly absorbed through PO route, no metabolism, excreted in kidneys and stool
      • allergy in 10% of people w/ the pen allergy
      • four generations: they all have the Cef- or Ceph- prefix.
  • Clindamycin
    • inhibits protein synthesis, Bacteriostatic
    • Narrow spectrum
    • Given with Tetracycline and Bactrim in MRSA
    • only for anaerobic infections such as in the gums, colon, sepsis
      • not effective in the CNS
    • Can give orally (IM,IV as well)
    • S/E: pseudomembranous colitis severe bloody diarrhea, Hepatic and renal toxicity, hypersensitivity
  • Erythromycin (macrolides)
    • Broad spectrum
    • inhibits bacterial protein synthesis
    • use is allergic to penicillin
    • for G+
    • long QT interval
    • S/E: GI upset, cholestatic hepatitis, superinfection
    • D/D: interacts with CCB, HIV protease inhibitors, and antifungal increase the serum levels of erythromycin
  • Fluoroquinolones (Ciprofloxacin) Metronidazole (Flagyl)
    • Broad spectrum
    • inhibits DNA gyrase in bacteria
    • Tendon rupture!!! do not give to kiddos under 18
    • undergo chelation just like tetracycline
  • Gentamycin
    • Aminoglycoside, Inhibits protein synthesis
    • for G- serious (aerobic) infections
    • nephro and ototoxicity
      • draw peak and trough levels to avoid toxicity
  • Penicillins
    • bactericidal in gram positive bacteria
    • safe to humans b/c we do not have cell walls
    • D/D interactions with anticoags increase bleeding, contraceptives with estrogen can be made ineffective when used with Penicillins.
    • beta lactam ring weakens the cell wall
      • beta lactamASE is used by some bacteria, breaks up the ring in the drug to make the drug ineffective
    • unstable absorption when taken orally
    • very thick and viscous IM needs to be givin Z track. it is thick and a lot of pressure is needed to administer.
    • few side effects, but 5% of the population has an allergic reaction
    • PenASE (beta lactamase) makes bacteria resistant to Penicillins
  • Classes of Pen. – Maybe just skim this, the individual drugs are not on the review list.
    • Pen G
      • Benzylpenicillin
        • narrow specturom, and sensitive to penASE
        • Bac-cidal to G+
        • prophylaxis in dental/invasive procedures for endocarditis and syphilis
    • Dicloxacillin
      • Narrow, PenASE resistant
      • Treat staph
    • Aminopenicillins
      • Ampicillin, Amoxicillin (broad spectrum)
      • G+ and some G- are treated
      • S/E: rash and Diarrhea
    • Extended spectrum Penicillins
      • Ticarcillin
      • Piperacillin
      • less important Carbenicillin indanyl, and mezlocillin
  • Ampicillin and sulbactam is Unasyn
  • Amoxicillin and Clavulanic acid is Augmentin
  • Sulfa drugs (sulfonamides) – Trimethoprim-Sulfamethoxazole (Bactrim)
    • Broad spectrum
    • inhibits folic acid to slow down growth
      • folic acid is used in the synthesis of Nucleic acid (DNA RNA and other nucleic acid strands)
      • (this is also why pregnant women should take folic acid supplements)
    • collect urine sample before giving any antibiotic
    • used in UTI G+ or G-
      • UTI is usually caused by e. coli
        • some elderly pts can have bacteria in the bladder and be asymptomatic and done not necessarily need to be treated.
    • Hypersensitivity reaction results in stevens- johnson syndrome
        • Bc it is a sulfa drug
  • Tetracyclines
  • Broad spectrum
  • Inhibit protein synthesis
  • Effective through PO route
  • for acne, lyme Dx, H. pylori, Cholera, Riskettsia, cholera
  • Can treat MRSA with Clindamycin, and Bactrim
  • chelation occurs when calcium, Iron, and magnesium containing supplements and foods inactivate the tetracycline and cause it to be inactive
    • do not take with meals!
    • one hour before or two hours after meals to avoid chelation
  • S/E: photosensitivity, brown teeth, not ok for mothers pregnant and breastfeeding moms, do not give to kiddos.
  • Vancomycin***
    • inhibit Cell wall synthesis
    • most used antibiotic in the US
    • for severe G+ infections: MRSA, C diff, prophylaxis endocarditis
    • ADME: PO is ok with this drug,
    • S/E:**altered taste, OTOTOXICITY**, redneck syndrome if given to quick IV
  • Antifungals
  • Amphotericin B
  • Broad spectrum  
      • Cell wall/membrane permeability is disrupted
        • humans have cell membranes…
        • binds -sterols which are also found in the human body (cholesterol) which causes the renal damage.
        • it is very toxic
      • used for SYSTEMIC mycoses that are potentially fatal, admin parenterally
      • S/E: infusion reaction fever and chills, nephrotoxic
      • ADME: can be found up to a year later in the pt body
  • Griseofulvin
  • still in the -azole class
  • just for SUPERFICIAL  (skin infections), not systemic
  • inhibits fungal mitosis
    • s/e: Insomnia, Rash and headache
  • Ketoconazole
    • used in less severe fungal reactions (fungistatic)
    • MOA is it inhibits the synthesis of ergosterol which is a part of the fungal cell membrane
      • this also affects the body’s sterols (sex hormones)
    • -conazols are all less toxic
  • Mycostatin (Nystatin)
    • Candidiasis only
    • It is in the form of a mouth wash
    • alters the permeability of the membrane
    • used for infant thrush often due to the low side effects.

Extras:

  • alprazolam (Xanax)
  • Anti anxiety
  • schedule IV, pregnancy class D
  • S/E: Dizzy, Lethargy, Drowsiness, CNS depression
  • grapefruit increases increases effects and the measurable levels of the drug
    • Estrogens
      • may increase risk of ALZ
      • inactivated with Gentamicin
      • contraceptives with estrogen can cause penicillin to be ineffective
    • Food and meds
  • Antacids, Fe, Ca, and Mg Causes chelation in tetracyclines and Fluoroquinolones all the previous + Alu, Zn, and sucralfate
  • Pre-op medication
      • reduce the bad effects of anesthesia
  • Atropine
        • Lomotil treats diarrhea from the use of anesthetics
        • also decreases secretions  
  • Baclofen
  • Anti-spastic
      • treats MM spasms from cerebral palsy, or Multiple sclerosis
      • Can cause seizures!
      • Increase CNS depression with opiates and MAO’s
        • MAO’s with this can also cause HYPOtension
      • Preg category C
    • Narcotics (pain), Benzos and barbs (anxiety), phenothiazines (nausea), MM relaxers.
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2 thoughts on “Pharmacology Study guide #3:

  1. FYI I think you have the relationship between Estrogen and Penicillin reversed. It should be that the use of Penicillin will cause Estrogen based contraceptives to be ineffective – not the other way around.

    Liked by 1 person

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