Exam 2 Flashcards

1
Q

Aspirin (ASA)

A

1st Gen NSAID
Mech: IRREVERSIBLE inhibition of COX!
Effects: Suppress inflamm - COX 2
Analgesia - COX 2
Antipyretic - COX 2
Reduce plt agg - COX 1
SE: Kidney impairment, Gastric ulcers, Bleeding, stimulates breathing -> potential resp alkalosis
General: Reye’s syndrome (ASA not given to children!)
Acute Poisoning:
1. Resp alkalosis -> resp acidosis
2. Hyperthermia
3. Dehydration
4. Electrolyte imbalances
5. Coma

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2
Q

Ibuprofen (Advil, Motrin)
Naproxen (Naprosyn, Aleve)

A

1st Gen NSAIDs
Mech: REVERSIBLE inhibition of COX
Effects: Suppress inflamm - COX 2
Analgesia - COX 2
Antipyretic - COX 2
SE: Gastric Ulcers
Bleeding
Kidney impairment
General: DOES NOT PROTECT AGAINST MI/STROKE

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3
Q

Ketorolac (Toradol)

A

Mech: suppression of prostaglandin synthesis
Effects: equiv pain relief to opiates w/o resp depression, tolerance, and abuse!
Small anti inflamm effect
SE: Gastric Ulcers
Bleeding
Kidney impairment
General

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4
Q

Celecoxib (Celebrex)

A

2nd Gen NSAID (only one!)
Mech: selective inhibition of COX 2 “coxib”
Effects: anti-inflamm & pain relief w/ reduced gastric risk!
SE: GI ulcers
Increase risk of MI, stroke
General: given for chronic inflamm, long term use!
Less GI effects

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5
Q

Acetaminophen (Tylenol)

A

Mech: Inhibits COX in the CNS ONLY! concentration to CNS explains why no anti-inflamm
Effects: Analgesic, Antipyretic
SE: W/ Alc induces CYP450 -> increases prod of toxic metabolite, depletes glutathione (converts NAPQI to non-toxic metabolite)
General: Acetylcyesteine (Mucomyst) converts toxic metabolite into non-toxic (replenishes glutathione)

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6
Q

Sumatriptan (Imitrex)
Rizatriptan (Maxalt)
“-triptan”

A

Serotonin Receptor Agonists
Mech: Stim sero receptors on cerebral vessels -> vasoconstriction
Also stim receptors on sensory neurons ->reduced release of inflamm neuropeptides
Effects: Used for migraine relief
SE: 50% of pts experience “heavy arms” or chest pressure due to thoracic vasoconstriction
General: Must avoid in preg! Teratogenic!
Cautious w/ other vasoconstriction meds

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7
Q

Ergotamine (ergomar)
Ergotamine + caffeine (Cafergot)

A

Mech: same as -triptans
Effects: prolonged use can lead to physical dependence, S&S similar to migraine attack!
SE: very well tolerated
10% experience nausea
Ergotism w/ prolonged use (periph vasc ischemia) think cold, numb, headache, severe leads to gangrene
General: teratogenic! dont use w/ -triptans

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8
Q

Morphine (strong)
Codeine (mod to strong)

Other:
Fentanyl
Meperidine (Demerol)
Methadone (Methadose)
Hydromorphone (Dilaudid)
Oxymorphone (Opana)

A

Pure Opioid Agonists

Mech: Bind to & activate Mu & Kappa receptors
Effects: relieves mod to severe pain w/o influencing other senses or causing LOC
SE: Resp depression
Constipation
Urinary retention
Ortho HypoT
Emesis
Cough suppression
Overdose :
1. Coma
2. Resp depress
3. Pinpoint pupils
Tx w/ opioid antag & mech vent
General: oral doses must be MUCH higher than other routes.
should NOT be given with CNS depressants, anticholinergics, HypoT meds

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9
Q

Hydrocodone (Vicodin)
Oxycodone (OxyCotin)
Codeine

A

Mod to Strong Opioid agonists

Mech: Bind to & activate Mu & Kappa receptors
Effects: lower intensity than morphine
SE: same as morphine
General: Same as morphine

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10
Q

Methadone (Methadose, Dolophine)

A

Pure opioid agonist

Mech: stim Mu & Kappa receptors.
Longer half life 22hrs
No peak/troughs of pain
Effects: used for opioid maintenance therapy (for a person not ready to withdraw)
SE: dependence on opioids, resp depress & life threatening arrhythmias in large doses
General: Can ONLY be Rx by certified opioid Tx program!

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11
Q

Pentazocine (Talwin)
Butorphanol (Stadol)

A

Agonist-Antagonist Opioids

Mech: Mu antagonist, Kappa agonist
Effects: used for mild to mod pain
SE: less severe than pure opioid SE’s
Limited resp depress
Can increase CV workload = chest pain
General: could see withdraw symptoms if also taking pure opioid agonist becus Mu are being blocked!

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12
Q

Buprenorphine (Suboxone)

A

Agonist-Antagonist Opioid

Mech: Mu partial agonist (suppresses craving), Kappa antagonist
Effects: used for opioid maintenance therapy (1/day dosing)
SE: lower risk of resp depress
General: can be prescribed in PCP office !

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13
Q

Naloxone (Narcan)

A

Opioid antagonist

Mech: competitive antagonist at opioid receptors, blocks opioid agonists
Effects: used for opioid overdose, life saving med! Lasts ~20min (book says 1hr)
Used post-op to break sedation
Used for neonatal resp depress
SE:
General: can induce withdrawal symptoms if given to someone w/ opioid dependence

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14
Q

Procaine (Novocain)
Lidocaine (Xylocaine)

A

Local Anesthetics

Mech: Block Na channels & prevent propagation of action potential
Block sensory & motor neurons
Effects: duration of anesthesia dependent on blood flow in region.
Often admin w/ Epi for vasocon = longer effect
SE: CNS excitation (seizure inducing)
Suppresses myocardium excitability = reduced conduction/heart block
General: Most of these SE not seen when admin SQ.
If given subdural during delivery, could reach baby!

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15
Q

Propofol (Diprivan)

A

Most widely used IV Anesthetic!

Mech: promotes release of GABA (keeps suppressing nerve impulse)
NO ANALGESIC EFFECT!
Effects: induction & maintanence of anesthesia, sedation while on mech vent
SE: profound resp depress!
HypoT
Risk for bacterial infection! Store 72
General: cannot be out unrefrigerated for >6hrs!
educate pt on green urine!

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16
Q

Etomidate (Amidate)

A

General Anesthetic

Mech: binds to GABA receptor & increases sensitivity to GABA
Effects: potential hypnotic used for induction of general anesthesia
NO ANALGESIC ACTION
SE: transient apnea!
HypoT
Electrolyte disturbances
General:

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17
Q

Ketamine (Ketalar)

A

General Anesthetic

Mech: Antagonizes NMDA receptor (Ca Channel)
Effects: used often for burn dressing changes
Produces state of “dissociative anesthesia”
SE: ~12% pts experience hallucinations post-op
General:

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18
Q

Cortisone
Hydrocortisone
Betamethasone (Celestone)
Dexamethasone (Decadron)
Prednisone (Deltasone)
Methylprednisolone (Medrol)

A

Glucocorticoids

Mech: Increase glucose levels, inhibit protein synthesis, mobilize fat (moon face, buffalo hump) , Mimic aldosterone = Na/water retention, K excretion
Inhibit prod of inflamm mediators
Suppress prolif of leukocytes
Effects: Tx Rheumatoid arthritis, SLE, IBD, allergic reactions, asthma, dermatology, suppression of transplant rejection
SE: CHAOS
Cushing’s syndrome (moon face/buffalo hump, fluid retention/HTN)
HypoK
Adrenal insufficiency if quick withdrawal
Osteoporosis
Suppressed immune system
General: Roid rage!
pt should be tapered off of steroid to avoid adverse effects!

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19
Q

Bismuth subsalicylate (Pepto-Bismol)

A

Mech: believed to disrupt bacterial cell wall
Effects: Can be used w/ amox to Tx H. Pylori
Used for diarrhea due to anti-secretory effect
SE: Grey/black stool, black tongue (harmless)
General:

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20
Q

Famotidine (Pepcid)
Cimetidine (Tagamet)
“-idine”

A

Histamine2 receptor antagonists

Mech: Blocks H2 receptors exclusively! No affect on H1 (allergies)
Normally H2 receptor provides cAMP to Proton-Pump to secrete stomach acid.
Effects: used for GERD, gastric/duodenal ulcers, Zollinger Ellison syndrome (hypersecretion of HCL from tumor)
SE: most common w/ Cimetidine
Anti-androgen effects (gynecomastia, reduced libido) not assoc w/ famotidine
CNS effects (confusion)
Pneumonia (buildup of bacteria in stomach)
General: Cimetidine inhibits CYP450 !

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21
Q

Misoprostol (Cytotec)

Analog of prostaglandin E1

A

Prostaglandin receptor antagonist
Mech: stim prostaglandin receptors on parietal cells to suppress prod of gastric acid
Effects: prev of gastric ulcers assoc w/ long use of NSAIDs
SE: Diarrhea, abdominal pain
Vaginal spotting or dysmenorrhea
General: contraindicated in preg women! Stim uterine contractions!

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22
Q

Omeprazole (Prilosec)
Esomeprazole (Nexium)
Pantoprazole (Protonix)

A

Proton Pump Inhibitors

Mech: Pro-drug that is activated in parietal cells of stomach. Inhibits the proton pump!
greater acid suppression than H2RAs!
Effects: lowers stomach acid, GERD & ulcers
SE: Very uncommon, headache, diarrhea, pneumonia by changing oral pharynx flora inhibiting acid secretion.
Rebound hypersecretion if quick cessation of PPI
General: Reduced acid secretion can influence absorption of anti-retrovirals

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23
Q

magnesium hydroxide (Milk of Magnesia)
Aluminum hydroxide/Magnesium hydroxide combo (Maalox)

A

Antacids

Mech: Alkaline compounds react w/ gastric acid to produce neutral salts
Raises stomach pH
Effects: Reduces destruction of gastric lining, reduces pepsin acitivity
SE: Usually affect the colon.
Milk of Mag causes diarrhea
Maalox can cause constipation
General:

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24
Q

Sucralfate (Carafate)

A

Mucosal protectant

Mech: NO ACID REDUCTION
Acts as a physical barrier!
In acidic environments converts to a gel that coats the stomach and adheres to ulcers
Effects:
SE: No known serious SEs
General: won’t be effective if taking an antacid. If stomach isn’t acidic, won’t convert to a gel

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25
Magnesium Hydroxide (Milk of Magnesia) Polyethylene glycol (MiraLax) Lactulose
Osmotic Laxatives **Mech:** poorly absorbed salts or carbs that pull water into intestines Softens fecal mass Feces expand & stretch colon Stimulates peristalsis **Effects:** **SE:** Loss of water, nausea, flatulence, Mg Hyd contraindicated in renal failure pt due to risk of tox (hyperMag) **General:**
26
Psyllium (Metamucil)
Bulk-forming laxative **Mech:** acts like natural fiber, swells in water, transforms into a gel, softens stool & increases bulk, swelling stretches colon stems peristalsis **Effects:** laxative **SE:** Rare, constipation & impaction if GI motility is interrupted **General:** PT SHOULD DRINK FULL GLASS OF WATER!
27
Docusate sodium (Colace)
Surfactant laxatives **Mech:** lowers surface tension of stool, allows water into stool, inhibits reabsorption of water from colon **Effects:** laxative **SE:** Rare **General:** PT SHOULD DRINK FULL GLASS OF WATER!
28
Disacodyl (Dulcolax, Feen-a-mint) Senna (Senokot) Castor Oil
Stimulant Laxatives **Mech:** stim intestinal motility, increase secretion of water & electrolytes into colon **Effects:** laxatives **SE:** Dependency, proctitis (inflamm of the anus) *typically only seen w/ repeated use* **General:**
29
Ondansetron (Zofran)
Antiemetic **Mech:** exerts effect by block serotonin in the pathway to the vomiting center **Effects:** anti-nausea **SE:** dizziness, risk for arrhythmia (Torsades de pointes) **General:**
30
Metoclopramide (Reglan)
Antieme*tic & Prokinetic **Mech:** Suppresses emesis by blocking serotonin AND dopamine in emesis pathway. Also enhances effect of ACh in upper GI tract (increases upper GI motility) **Effects:** **SE:** *usually only w/ high dose & prolonged use* Tardive dyskinesia & possible neuroleptic malignant syndrome (NMS, v similar to malignant hyperthermia) Sedation **General:**
31
Scopolamine (Scopoderm)
Antiemetic **Mech:** Blocks muscarinic receptors on pathway to vomiting center **Effects:** Used for motion sickness! **SE:** anti-cholinergic effects (dry mouth, constipation, blurry vision) **General:**
32
Meclizine (Antivert) Dimenhydrinate (Dramamine)
Antiemetic **Mech:** Blocks histamine receptors on pathway to vomiting center Also blocks muscarinic receptors to a lessor degree **Effects:** Used for motion sickness! **SE:** Anti-cholinergic & ant-histamine SE’s **General:**
33
Sulfasalazine (Azulfidine)
5-aminosalicylates **Mech:** Reduces inflamm by suppressing prostaglandin synthesis by inhibiting COX **Effects:** Used for Tx of acute IBS attack **SE:** Nausea, fever, rash **General:**
34
Budesonide (Entocort) Prednisone (Deltasone)
Glucocorticoids **Mech:** Inhibits protein synthesis, inhibits synth of chem mediators (prosta, Leuko, histamine) **Effects:** anti-inflamm, reduce swelling (decreases vasodilation), reduces pain **SE:** *usually only in long term use or high doses* CHAOS, psychologic disturbances **General:**
35
Infliximab (Remicade) “-mab” = Mono-clonal antibody
Immunomodulators **Mech:** Binds to & neutralizes TNF-a , reduces inflamm **Effects:** IV Admin only! **SE:** Immunosuppression increases risk of infection, infusion reaction risk! **General:** Tell pt to report sore throat or fever!
36
Adalimumab (Humira)
Immunomodulator **Mech:** Binds to & neutralizes TNF-a, reduces inflamm **Effects:** SQ ADMIN **SE:** Risk of infection, injection site reaction **General:** Tell pt to report sore throat or fever! Pt edu on how to admin SQ injection
37
Cyclosporine (Neoral, Sandimmune)
Immunomodulator **Mech:** Suppresses prod of interleukens & other cytokines, reduces prolif of B and cyto T cells **Effects:** Used to prevent organ transplant rejection **SE:** increased risk of infection, *nephrotoxicity* **General:** tell pt to report sore throat or fever
38
Heparin *unfractionated heparin*
**Mech:** increases the activity of anti-thrombin! -> inactivates thrombin & factor Xa Works very quick! **Effects:** Admin parenteral ONLY! Best for venous thrombi Good for conditions that require rapid response (PE, DVT, MI) Doesn’t cross placenta or BBB *preferred in preg* **SE:** Hemorrhage!! (Dark stools, lumbar/abdominal/pelvic pain), spinal/epidural hematoma Heparin-induced thrombocytopenia (prod of abs against heparin-plt complex) **General:** PROTAMINE SULFATE IS ANTIDOTE!! Admin slow IV push 1mg neutralizes 100u heparin Monitor aPTT labs Normal Essex Therapeutic 1.5-2.5x normal (60-80sec)
39
Enoxaparin (Lovenox) “No Xa” *Low molecular weight heparin*
**Mech:** Neutralizes factor Xa better! Increases the activity of anti-thrombin resulting in less thrombin & Xa. Fast acting! **Effects:** Long half-life (only admin 1-2x/day) Good for DVT prev post op or Tx of estab DVT Given prophylactic for CV issues **SE:** Bleeding! Risk much lower than heparin **General:** more expensive! Pre-filled syringes. TX OVERDOSE W/ PROTAMINE SULFATE!
40
Fondaparinux (Arixtra)
Anticoag **Mech:** binds to anti-thrombin, complex inactivates factor Xa, prevents Xa from converting prothrombin to thrombin **Effects:** Admin SQ **SE:** Bleeding! Use caution in renal failure pts! Pt w/ epidural cath may experience hematoma! **General:** pre-filled syringes
41
Warfarin (Coumadin)
**Mech:** Blocks activation of vit K! Reduces synthesis of 4 vit K dependent clotting factors (specifically prothrombin) Delayed onset of action cus it does not affect clotting factors already in circulation!! 99% protein bound on first dose! **Effects:** Admin PO. Long term prophylaxis of thrombosis in aFIB, art valves, hx of PE. Peak effect not seen until 3-5 days. Long half life! Remains effective up to 5 days after cessation **SE:** bleeding! Risk much lower than heparin! Monitor labs for INR! Weekly to start, once therapeutic levels, monthly. Therapeutic INR = 2-3 Mech heart valve = 3-4.5 **General:** ANTIDOTE IS VIT K!! Admin PO or IV MUST BE ADMIN SLOWLY OVER 1HR TO PREVENT ANAPHYLAXIS! Pt goes for labs to check INR every month Change in Vit K intake can influence how well it works. Edu pt to not change vit K habits
42
Dabigatran etexilate (Pradaxa)
Direct Thrombin Inhibitor (DTI) **Mech:** Binds to thrombin, prevents it from converting fibrinogen to fibrin Faster onset than warfarin! **Effects:** Admin PO. No need to monitor drug levels!! Fewer food-drug interactions! Same dose given regardless of weight or age Used to prev recurrent DVT or PE **SE:** Bleeding but lower risk! GI disturbances in 35% of pts!! Can produce GERD, gastric ulcer (reduce risk by taking w/ food) **General:** PRAXBIND IS ANTIDOTE! (Mono ab) always a risk for anaphylaxis!
43
Rivaroxaban (Xarelto) Apixaban (Eliquis) (-xaban)
Direct Factor Xa Inhibitors **Mech:** binds to factor Xa, prevents conversion of prothrombin to thrombin **Effects:** admin PO. Faster onset than warfarin. Used for DVT prev following knee/hip sx. Tx or prev of DVT/PE **SE:** much lower bleeding risk than warfarin! Spinal/epidural hema, (hold meds for sev hours before & after lumbar puncture) **General:** No need to monitor labs! ANDEXXA IS ANTIDOTE!!
44
Clopidogrel (Plavix) Plasugrel (Effient) Ticagrelor (Brilinta) (-grel)
ADP receptor antagonists , anti-plt med **Mech:** Blocks P2Y12 ADP receptors on plts! Prevents ADP from binding & activating plt! *Irreversible! Lasts for life of plt!* Pro-drug, activated by CYP450! **Effects:** Admin PO, prev occlusion of Coronary Artery Stents! **SE:** Bleeding! (Risk lower than ASA) GI & Intracranial bleeds most common! Abdominal pain Use caution w/ other ACs MUST BE STOPPED 5DAYS PRIOR TO SX! **General:** PPIs can inhibit CYP450 which would inactivate these drugs!
45
Tirofiban (Aggrastat) Eptifatide (Integrilin) *”Super Aspirin”*
Glycoprotein IIb/ IIIa receptor antagonists **Mech:** Blocks Gp IIb/IIIa receptors on plts & prev fibrinogen from attaching -> prev plt agg **Effects:** Admin IV, used for short term Tx of ischemic events in pts w/ ACS s/p PCI **SE:** Bleeding! **General:**
46
Alteplase (Activase) Aka *tPA, synthetic version of naturally occurring tPA (tissue plasminogen activator)
Thrombolytic Med “clot buster” **Mech:** Binds to plasminogen, promotes conversion to Plasmin, Plasmin digests fibrin clots! **Effects:** admin w/ IV cath place RIGHT at the clot! Used for MI, PE, ischemic stroke! **SE:** Bleeding! Especially in intracranial area! Hemostasis restored w/ blood products (packed RBCs, FFP) If that doesn’t work, antidote is Amicar! **General:** Reduce IV and SQ injections to reduce risk of bleeding! Minimize invasive procedures! Use caution if used w/ warfarin or anti-plt meds!
47
Budesonide/Formoterol (Pulmicort) Fluticasone/Salmeterol (Flovent)
Inhaled corticosteroids **Mech:** reduces synth of inflamm mediators (leukotrienes, histamine, etc) Reduces recruitment of inflamm cells **Effects:** Used for prophylaxis against inflammation in asthma! Common controller med! **SE:** Oropharyngeal candidiasis (thrush) *pts should rinse mouth & gargle warm water after to minimize risk* Systemic: CHAOS **General:** small pop develops neuropsychiatric effects
48
Montelukast (Singulair) Zafirlukast (Accolate)
Leukotriene Receptor Antagonists (LTRA) **Mech:** suppress effects of leukotrienes = less inflamm **Effects:** Admin PO, Controller med! **SE:** Headache & GI most common, small pop develops neuropsychiatric effects **General:**
49
Cromolyn
Mast Cell Stabilizer **Mech:** Prevents mast cell from releasing histamine! **Effects:** SAFEST OF ALL ASTHMA MEDS!! Admin inhalation. Used for prophylaxis NOT immed tx **SE:** tolerated very well **General:** Very expensive!
50
Albuterol (Ventolin, Proventil) Levalbuterol (Xopenex) Terbutaline (Brethine) (-terol)
Bronchodilators Reliver/rescue meds Short-acting beta agonists (SABA) **Mech:** Stim Beta 2 receptors, causes bronchodilation **Effects:** Usually only taken PRN **SE:** Usually tolerated well, minimal systemic absorption unless taken PO = tachy & tremor (beta 2 activation on skeletal muscle) **General:**
51
Formoterol (Foradil) Salmeterol (Serevent Discus)
Long-acting beta agonists (LABA) **Mech:** Stim beta 2 receptors , causes bronchodilation **Effects:** Taken on a fixed sched! Preferred over SABA for COPD tx! Must be combined w/ GC for tx of asthma. Tx asthma & COPD **SE:** IF LABAs ARE NOT COMBINED W/ INHALED CORTICOSTERIOD, MORE LETHAL! **General:**
52
Theophylline (Theochron, Theolair)
Methylxanthines **Mech:** Promotes relaxation of bronchial smooth muscle **Effects:** occasionally used to tx asthma. Admin PO or IV, narrow Thera range 10-20mcg/mL **SE:** Overall well tolerated, GI disturbances, CNS excitation **General:** Educate pt that **caffeine** may intensify effects!
53
Ipratropium bromide (Atrovent) Tiotropium (Spiriva) (-tropium)
Long acting muscarinic antagonists (LAMA) **Mech:** Prevents ACh from binding, causes unopposed bronchodilation (& other anti-cholinergic effects if systemic) **Effects:** Used for tx of asthma! Often admin w/ a beta 2 agonist! **SE:** Anti-cholinergic SE’s (dry mouth, nasal congestion, headache, cough) **General:**
54
1st Gen (Sedating) Diphenhydramine (Benadryl) 2nd Gen Cetirizine (Zyrtec) Levocetirizine (Xyzal) Fexofenadine (Allegra) Loratadine (Claritin)
Antihistamines **Mech:** Bind to H1 receptors & prevent them from being activated by histamine, when H1 receptors in brain are blocked causes drowsiness! 2nd Gens do NOT cross BBB **Effects:** 1st line tx for allergic rhinitis **SE:** Mild sedation w/ Benadryl, urinary retention, dry mouth, constipation **General:** best when taken prophylactically
55
Budesonide (Rhinocort) Triamcinolone (Nasacort) Fluticasone (Flonase)
Intranasal Glucocorticoids **Mech:** Bind to glucocorticoid receptors on cell surface. Promotes prod of proteins that suppress immune system. **Effects:** Most effective Tx of seasonal rhinitis!! **SE:** Drying of the nasal mucosa, Epistaxis (bloody nose), sore throat Systemic = CHAOS s&s **General:** pts may report unpleasant taste in mouth
56
Codeine (Robutussin)
Opioid antitussive Most effective cough suppressant available!* **Mech:** bind to opioid receptors in CNS to elevate cough threshold **Effects:** cough suppressant **SE:** Resp depress **General:** Not rec for children or people w/ reduced resp capacity
57
Dextromethorphan (Robutussin, Delsym)
Non-opioid anti-tussives **Mech:** Works in CNS to elevate cough threshold Derivative of opioids **Effects:** cough suppressant **SE:** may cause mild inebriation **General:** advise pt to avoid activities that require mental alterness
58
Guaifenesin (Mucinex)
Expectorant **Mech:** believed to improve water retention in resp tract , reduces viscosity of mucous **Effects:** **SE:** Nausea/vomiting, dizziness, drowsiness **General:**
59
Acetylcysteine (Mucomyst)
Mucolytic **Mech:** binds directly to mucous to reduce viscosity **Effects:** Admin by nebulizer **SE:** Nausea/vomiting, chest tightness, bronchospasm, urticaria **General:** Use w/ caution in people w/ asthma!!
60
Gum, Nicotrol (nasal spray & inhalant by Rx) Lozenge (Commit) Transdermal patch (Habitrol)
Nicotine replacement therapy **Mech:** deliver nicotine at a lower dose and slower rate than tobacco containing products, reduces nicotine withdrawal symptoms **Effects:** Rec for people who smoke > 20 cigs/day, who smoke within 30min of awakening, who have failed to quit in the past. **SE:** Skin irritation common for patch! Contraindicated in pregnancy! **General:** Gum improves cessation rates 40-60%
61
Varenicline (Chantix)
**Mech:** Partial agonist at nicotinic receptors! Minimizes withdrawal symptoms, nicotinic receptor cannot Stim release of dopamine = less stimulus of reward center!! **Effects:** **SE:** Nausea, disturbed sleep **General:** Very expensive!! Typically not covered by cessation programs
62
Cyclosporine (Sandimmune, Neoral)
Calcineurin inhibitors *Most effective immunosuppressants available!* **Mech:** inhibit calcineurin, suppress prod of IL-2 (activates cytotoxic T cells & B cells) **Effects:** drug of choice for prev of organ rejection from donor! **SE:** Nephrotoxicity!! (Monitor BUN & creatinine) Infection Grapefruit juice inhibits metabolism, can increase levels by 200%! **General:** Pt should report sore threat / fever immed! Highly influenced by drugs that influence metabolism of CYP450
63
Tacrolimus (Prograf)
**Mech:** Inhibits calcineurin, suppresses prod of IL-2 (activates cytotoxic T cells & B cells) **Effects:** More effective than Cyclosporine BUT more TOXIC! Used for prophylaxis or organ rejection **SE:** NEPHROTOXICITY, Infection, Neurotoxicity (headache, tremor, insomnia), GI effects , HTN, HyperK **General:** Pt should report sore throat, fever immediately! Highly influenced by drugs that influence CYP450
64
Adalimumab (Humira) Entanercept (Enbrel) Infliximab (Remicade)
Disease-modifying anti-rheumatic drugs (DMARDs) *TNF antagonists* **Mech:** binds to TNF-a & neutralizes it, prevents from Stim inflamm **Effects:** Used to tx rheumatoid arthritis Admin IV or SQ (often auto inject pen) **SE:** Injection site reactions, risk for serious infections (fungal, TB, legionella, pneumonia, react of latent HepB) **General:** Pt needs to report any S&S of infection, avoid live vaccines, edu about latent disease going active
65
Rituximab (Rituxan)
DMARDs *B-lymphocyte depleting agents* **Mech:** monoclonal abs that bind to a receptor exclusive to B-lymphocytes, promotes immune attack against b-lymph = b-lymph destroyed **Effects:** IV ADMIN ONLY! **SE:** SEVERE INFUSION REACTIONS (HypoT, bronchospasm, angioedema, shock) **Pre-med w/ antihistamine & acetaminophen** Skin reactions including Stevens-Johnson syndrome (SJS, rare cutaneous reaction to meds. cells take portion of med & bind it to MHC 1, targeted & destroyed by body) **General:**
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Acyclovir (Zovirax)
**Mech:** inhibits replication by suppressing synthesis of viral RNA **Effects:** 1st choice for infections by HSV, VZV, CMV. Admin many routes **SE:** IV: phlebitis & inflamm @ injection site, Nephrotoxicity! Pt needs to stay hydrated!!! Neuro tox (tremors) esp in renal fail pts PO: mild, GI & headache **General:** resistance is possible in immunocompromised pts!
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Valacyclovir (Valtrex)
*Prodrug of Acycolvir* **Mech:** Inhibits replication by suppressing synth of viral RNA **Effects:** ONLY USE IN IMMUNOCOMPETENT INDIVIDUALS! **SE:** Same as Acyclovir PLUS Thrombotic thrombocytopenic purpura (TTP) in immunocomp pt! **General:**
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Ganciclovir (Cytovene)
**Mech:** suppresses rep of viral DNA **Effects:** used for prev & tx of CMV in immunocompromised host **SE:** Bone marrow suppression!!! Can cause granulocytopenia & thrombocytopenia Reproductive tox is big concern! **General:** 85% of pop are carriers of CMV
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Interferon Alfa
Hepatitis Drug **Mech:** prev viral entry into cell, prev synth of viral mRNA, prev synth of viral proteins, protein assemb, and protein release **Effects:** synthetic version of nat occur compound. Almost always SQ! PEGinterferon is the long-acting version of the drug! **SE:** Flu like syndrome!! Depression & suicidal ideation Thyroid dysfunction Heart damage **General:**
70
Ribavirin (Rebetrol) *has a look-a-like med*
**Mech:** unknown, nucleoside analog? Joins growing nucleotide chain, blocks the continuation of forming DNA **Effects:** Commonly given w/ PEGinterferon, broad spectrum of antiviral activity **SE:** Hemolytic anemia, fetal injury!! **General:** **Contraindicated in preg, use 2 forms of BC!!**
71
Boceprevir (Victrelis)
**Mech:** Inhibits protease (enzyme nec for maturation of a virus) **Effects:** Given in conjunction with/ PEGinterferon & ribavirin, GREATLY enhances overall antiviral effects **SE:** Generally well tolerated, mild fatigue, nausea, chills, altered taste **General:**
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Ledipasvir/sofosbuvir (Harvoni)
**Mech:** Block 2 enzymes necessary for viral rep! **Effects:** Tx hepatitis **SE:** Headache & fatigue! Brady if taken with amiodarone! **General:**
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Sofosbuvir/Velpatasvir (Epclusa)
**Mech:** Blocks 2 enzymes necessary for viral rep **Effects:** Used to Tx hep **SE:** Headache & fatigue PLUS react of latent hep B **General:** Brady if taken w/ amiodarone
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Oseltamivir (Tamiflu)
Neuraminidase inhibitor **Mech:** Inhibits neuraminidase (respon for seaparation of virus from host cell) Newly formed viruses cannot bud off! **Effects:** MUST be taken WITHIN 48HRS after symptom onset! Also shown to be effective in PREVENTING influenza **SE:** HALLUCINATION AND SI HAVE BEEN REPORTED IN CHILDREN!!! **General:**
75
Flu vaccine - inactivated virus
**Mech:** given inactivated virus to develop immunity **Effects:** protection begins 1-2 weeks after inoculation, lasts 6 months Admin IM or intradermal **SE:** soreness at site, fever, malaise if not vaxx in past Small risk of Guillain-Barré syndrome (ascending paralysis, destruction of myelin sheath) **General:** instruct pt to get vaxx in Oct/Nov to be covered for heigh of flu season. Need to know if pt has egg allergy CANNOT GET VAXX IF CURRENT FEVER!
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Flu vaccine - live, attenuated virus
**Mech:** introduced to live, weakened virus **Effects:** Protection begins 1-2 weeks post inoculation, lasts 6mo **SE:** CANNOT BE GIVEN TO IMMUNOCOMPROMISED! Runny nose, nasal congestion, cough **General:** CANNOT GET VAXX IF CURRENT FEVER
77
Zidovudine (Retrovir) Lamivudine (Epivir)
Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (NRTIs) **Mech:** Chem relatives of nucleosides & nucleotides. Suppresses synth of viral DNA by incorporating into chain, blocking further growth **Effects:** mainstay of HIV therapy **SE:** BONE MARROW SUPPRESSION!! May need blood transfusions Lactic acidosis (enzyme that breaks down LA can’t form) and hepatomegaly **General:** use of additional drugs that suppress bone marrow can increase risk of anemia & neutropenia
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Efavirenz (Sustiva)
Non-NRTIs (NNRTIs) **Mech:** Binds DIRECTLY to HIV reverse transcriptase, inactivating enzyme! **Effects:** no structural relationship to nucelosides **SE:** If rash **STOP IMMEDIATELY!** CNS symp like dizziness, drowsiness Teratogenic!! **General:**
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Ritonavir (Norvir) Lopinavir/Ritonavir (Kaletra)
Protease Inhibitors (PIs) **Mech:** prev HIV protease from cleaving the long protein chain into the individual enzymes & structural proteins = virus remain immature & non-infectious! **Effects:** Often combined with NRTIs to reduce viral load to undetectable levels! **SE:** INHIBITS CYP450! We’ll tolerated, diarrhea, nausea, headache, prolongs segments of EKG **General:**
80
Raltegravir (Isentress)
Integrase strand transfer inhibitor (INSTI) aka Integrase inhibitor **Mech:** Inhibits integrase, HIV DNA cannot be incorporated into DNA of host! **Effects:** only drug in this cat! **SE:** Insomnia, headache, severe hypersensitivity (SJS) rare **General:**
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Enfuvirtide (Fuzeon)
HIV Fusion Inhibitor **Mech:** Prev HIV envelope from fusing w/ cell membrane of host cell. Blocks entry of HIV into host cell **Effects:** 2x/day SQ Injections! Expensive! **SE:** Injection site reaction in 98% of pts!! Teratogenic Increased pneumonia risk Hypersensitivity **General:**
82
Truvada or Descovy (emtricitabine-tenofovir)
PrEP **Mech:** Both drugs are nucleotide/nuceloside reverse transcriptase inhibitors Prevents conversion of viral RNA to viral DNA **Effects:** Descovy only approved for people AMAB **SE:** Nephrotoxicity, Hepatotoxicity! Lactic acidosis Osteoporosis **General:**
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Penicillin G Nafcillin Ampicillin Amoxicillin Piperacillin - *effective against Pseudomonas*
**Mech:** PCNs are bactericidal! Bind to PCN binding protein (PBPs) in cell membrane Inhibit enzymes that synth cell walls! Activates autolysins ! **Effects:** PCN G tends to be very safe, cannot be given PO! All PCNs can be administered IM but vary in absorption Benzathine PCN G abosrbed SLOWLY over weeks Amox & Amp have additional SEs of diarrhea **SE:** ALLERGIC REACTION IS #1 CONCERN! Reaction ranges from rash-anaphylaxis. Tx for reaction is Epi 1:1000 concentration IM! IF ANAPHYL TO PCNs, WILL NOT GIVE CEPHALOSPORINS! **General:** Bacteria can be resistant to PCNs, thick outer membrane of Gram Neg cannot be pen by PCN Beta lactamase, enzyme prod by bacteria that destroys betal-lactamase ring of PCN MRSA creates PBPs w/ poor affinity to PCN
84
Ampicillin/Sulbactam (Unasyn) Amoxicillin/Clavulanate (Augmentin) Piperacillin/Tazobactam (Zosyn)
PCN combine w/ B-Lactamse inhibitor **Mech:** Prev destruction of b-lactam ring by binding to b-lactamase **Effects:** if pt doesn’t improve after starting w/ abx, you switch to one of these! **SE:** **General:**
85
1st Gen: Cephalexin (Keflex) 2nd Gen: Cefaclor (Ceclor) 3rd Gen: Ceftriaxone (Rocephin) 4th Gen: Cefipime (Maxipime) 5th Gen: Ceftaroline (Teflaro) *Only one w/ activity to MRSA*
Cephalosporins (Cef- or ceph-) **Mech:** As gen’s increase: better at resisting b-lactamase, better activity against gram neg bacteria & anaerobes, increased ability to cross BBB **Effects:** Need to consider pts renal fx! **SE:** **BAT** = Bleeding (increases Vit K metab) Allergic reaction (usually rash, Ana is rare) Thrombophelbitis (rotate IV infusion sites) **General:** Interaction with Acl!!! Disulfiram reaction (strong adverse reaction to alc, makes pt sick)
86
Imipenem (Primaxin)
Carbapenems (-penem) **Mech:** Bactericidal , binds to PBPs = weakens cell wall & causes lysis **Effects:** Must be given IV! **SE:** GI effects most common! **General:**
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Aztreonam (Azactam)
Monobactams **Mech:** Binds to PBPs = bactericidal, *highly resistant to b-lactamase* **Effects:** can only be given IV or IM **SE:** pain at injection site Thrombophelbitis at IV site **General:**
88
Vancomycin
**Mech:** Binds to molecules that are precursors to cell wall synth **Effects:** **Most widely used antibiotic in US hospitals!** Typically used to Tx C.diff infections (admin PO) and MRSA Admin by slow IV infusion except for Tx of c.diff (PO) **SE:** Renal failure, “Vanco flushing syndrome” stim release of histamine, vasodilation and flushing Thrombophelbitis **General:**
89
Getamicin Tobramycin Amikacin (Amikin)
Aminoglycosides *Bactericidal inhibitors of protein synthesis* **Mech:** Bind to ribosome w/ 3 effects: Inhibit onset of protein synthesis Premature term of protein synthesis Prod of abnormal code leading to cell membrane lysis/failure **Effects:** monitoring of drug levels is important!! **elevated TROUGH is assoc w/ toxicity!!** Peak measure 1hr after admin Trough 30min before admin **SE:** Serious tox!!! Especially in kidney & ear! Ototoxicity = high pitched tinnitus Nephrotox = acute tubular necrosis, usually reversible **General:** HIGHLY polar so not absorbed in gut, can’t cross BBB! AMNO = Aerobic organisms only Mostly bactericidal Inhibits protein synthesis/IV only Nephrotox/Neuro musc block Ototoxicity
90
Tetracycline Doxycycline (Vibramycin)
Tetracyclines (-cycline) **Mech:** Bind to ribosome, prevents binding of tRNA, chain of amino acids cannot be built , growth of bacteria is stopped **Effects:** **1st LINE TX FOR: CHALMYDIA TRACHOMATIS, LYME DISEASE, BACILLUS ANTRACIS, ROCKY MOUNTAIN SPOTTED FEVER, H. PYLORI** **SE:** Binds to Ca in developing teeth causing GREY STAINING! DO NOT GIVE TO CHILDREN UNDER 8yo! Hepato * Nephrotox Suprainfection **General:** Binds to Ca products (dairy) and inactivates abx! Edu pt to not take w/ milk or dairy, don’t take with Ca supplements, or iron supplements
91
Erythromycin Azithromycin (Zithromax) Clarithromycin (Biaxin)
Macrolides (-thromycin) **Mech:** broad spectrum similar to PCNs Binds to ribosome and prevents chain of amino acids being built **Effects:** **1st LINE DRUG FOR: LEGIONELLA PNEUMONIA, BORDETELLA PERTUSSIS, CORYNEBACTERIUM DIPHTHERIAE **SE:** GI irritation, prolong QT **General:** INHIBITS CYP450!! Can lead to Dig tox, increased bleeding w/ warfarin!
92
Clindamycin (Cleocin)
**Mech:** Binds to ribosome & prev chain of amino acids **Effects:** **SE:** POTENTIALLY FATAL C.DIFF ASSOC DIARRHEA!!!! SUPRAINFECTION! **General:**
93
Linezolid (Zyvox)
**Mech:** Binds to ribosome prev chain of amino acids **Effects:** RESERVED FOR MULTI-DRUG RESISTANT ORGANISMS !!! Like MRSA, VRE! **SE:** GI irritation **General:**
94
Sulfamethoxazole
Sulfonamides (Sulfa drugs) **Mech:** Structurally similar to PABA, Sulfonamide is incorporated into molecule instead of PABA, stops prod of folic acid!! **Effects:** usually used to Tx UTIs **SE:** Hypersensitivity = mild rash & fever most common **Photosensitivity** Hemolytic anemia! Kernicterus (bilirubin in brain) SJS can occur **General:** Inhibits hepatic metab of some drugs like warfarin, cross hypersensitivity with other sulfur-based drugs
95
Trimethoprim/Sulfamethoxazole (Bactrim)
**Mech:** Interfers w/ consecutive steps in synth of folic acid **Effects:** Used for UTIs + pneumocystis pneumonia **SE:** Fetal malformation!! Hemolytic anemia! HyperK! GI disturb , itching & rash **General:**
96
Ciprofloxacin (Cipro) Levofloxacin (Levaquin) Moxifloxacin (Avelox)
Fluoroquinolones (-floxacin) **Mech:** inhibits 2 bacterial enzymes responsible for DNA rep & cell division **Effects:** CYP450 inhibitor!!! **SE:** TENDON RUPTURE!! ACHILLES TENDON!! Phototoxicity! Mild GI **General:** tell pt to not take with milk, dairy, Ca supplements, iron, antacids
97
Metronidazole (Flagyl)
**Mech:** Prodrug is taken in by anaerobic organisms, converted into active form, breaks DNA strands **Effects:** ONLY EFFECTIVE AGAINST ANAEROBES!!! **SE:** Metallic taste in mouth, Hypersensitivty reaction (SJS) **General:** Disulfiram like reaction w/ alc!
98
Isoniazid (Nydrazid) *aka INH*
TB Drug **Mech:** Not clear, believed to reduce prod of important component of cell wall **Effects:** **SE:** Hepatox , peripheral neuropathy, CNS effects (Seizures) **General:**
99
Rifampin (Rifadin)
TB Drug **Mech:** Inhibits DNA dependent RNA polymerases , blocks RNA synthesis , Blocks protein synthesis **Effects:** INDUCES CYP450!!! Lower warfarin level Lower dig level Lower BC level **SE:** DISCOLORATION OF BODY FLUIDS : red/orange color to urine, sweat, saliva, tears, harmless. hepatox **General:**
100
Amphotericin-B (Amphotec)
Polyene anti-fungal **Mech:** binds to ergosterol on the surface of fungal cell membrane, increased permeability **Effects:** must be admin IV (poor GI absorption) **SE:** Binds to sterols on mammalian cells like cholesterol!! Infusion reactions Nephrotox HypoK **General:** reduce SEs by pre-Tx w/ Benadryl & acetaminophen! **Nystatin (Mycostatin)** is in the same fam but MUCH less toxic (topical)
101
Fluconazole (Diflucan) Ketoconazole (Nizoral) Miconazole (Monistat)
Azole antifungals (-conazole) **Mech:** inhibits prod of ergosterol, necessary for fungal cell membranes Results in leakage & rupture **Effects:** better alt to Ampotericin B for SYSTEMIC fungal infections! Slightly less toxic and admin PO! **SE:** INHIBITS CYP450!!! GI Disturbances **General:**