Term
| Examples of OTC Bronchodilators |
|
Definition
| Primatine Mist (epinephrine) |
|
|
Term
| IND for OTC Bronchodilators |
|
Definition
| May be used for asthma, but not an optimal drug |
|
|
Term
| MOA of OTC Bronchodilators |
|
Definition
| B1 and B2 short-acting agonist |
|
|
Term
| SE of OTC Bronchodilators |
|
Definition
| If overused, you'll see excessive B1 effects (tachycardia, arrhythmias, and worsening angina) |
|
|
Term
| Example of Short-Acting B2- Adrenergic Agonists |
|
Definition
| Albuterol (Ventolin, Proventil, etc.) |
|
|
Term
| IND for Short-Acting B2-Adrenergic Agonists |
|
Definition
| For episodic, "quick relief" of wheezing in asthma and COPD |
|
|
Term
| MOA of Short-Acting B2-Adrenergic Agonists |
|
Definition
| B2 agonist primarily - activation of these receptors causes bronchial smooth m. relaxation with bronchodilatation. Note - these are NOT anti-inflammatory agents. |
|
|
Term
| SE of Short-Acting B2-Adrenergic Agonists |
|
Definition
| If overused, you may have some B1 effects |
|
|
Term
| Examples of Long-Acting B2-Adrenergic Agonists |
|
Definition
| Salmeterol (Serevent) - available as an inhaler or dry powder; Fomoterol (Foradil aerolizer) - dry powder formulation |
|
|
Term
| MOA of Long-Acting B2-Adrenergic Agonists |
|
Definition
| Salmeterol MOA: has a long half-life due to high lipid solubility - slowly released to receptors; otherwise MOA is similar to that of Short-acting B2-adrenergic agonists |
|
|
Term
| IND for Long-Acting B2-Adrenergic Agonists |
|
Definition
| For "maintenance Rx" of moderate or severe persistent asthma and COPD; and every 12 hour or bid regimen improves compliance; Note - this is NOT monotherapy for asthma, you need to combine it with an anti-inflammatory agent |
|
|
Term
| SE of Long-Acting B2-Adrenergic Agonists |
|
Definition
| If overused, you may see tachycardia and/or irregular HR |
|
|
Term
| IND for Anticholinergic Agents |
|
Definition
|
|
Term
| Examples of Anticholinergic Agents |
|
Definition
| Ipratropium (Atrovent), Tiotropium (Spiriva) |
|
|
Term
| SE of Anticholinergic Agents |
|
Definition
| Anticholinergic SE of dry mouth and urinary retention, especially in men with BPH. Recently, concerns have been raised in meta-analyses about increased risk of CV deaths, MI or stroke in patients on long-term Rx |
|
|
Term
|
Definition
| Short-acting, given 4x/day; this inhaled anticholinergic agent competitively blocks muscarinic receptors in the airways and prevents bronchoconstriction mediated by vagal discharge |
|
|
Term
|
Definition
| "Maintenance drug" in COPD to prevent bronchospasm; since it's given 4x/day, the once daily prep, tiotropium, is often preferred; Not FDA-approved for use in asthma in the out-patient department |
|
|
Term
|
Definition
| AKA: Combivent; FYI - be aware that you may see this agent used 4x/day in COPD, but do you want to use a short-acting B2-adrenergic agonist 4x/day? Probably not - often salmeterol, the long-acting B2-adrenergic agonist prep used 2x/day AND ipratropium 4x/day or tiotropium once a day, used separately would be preferred. |
|
|
Term
|
Definition
| Like ipratropium, it binds with high affinity to muscarinic receptors in airway smooth m. cells and mucous glands, inhibiting the bronchoconstrictive and secretory effects of acetylcholine |
|
|
Term
|
Definition
| For once-daily maintenance Rx of bronchospasm in COPD |
|
|
Term
| Examples of Inhaled Corticosteroids |
|
Definition
| fluticasone (Flovent), beclemethasone (Vanceril) |
|
|
Term
| MOA of Inhaled Corticosteroids |
|
Definition
| The key anti-inflammatory agents in asthma Rx; these drugs decrease eosinophils, cytokines, leukotriene release, capillary permeability and mucosal edema, providing an anti-inflammatory effect; it takes a few days to achieve maximum effect |
|
|
Term
| IND for Inhaled Corticosteroids |
|
Definition
| Asthma - NOT for relief of acute sxs (because it takes days to work); for maintenance Rx in mild-moderate persistent asthma (i.e. in patients with daily asthma sxs and/or bronchospasm requiring a short-acting B2-adrenergic agonist >3x/wk). In COPD - their role is evolving: before the TORCH study, ICS were felt to be useful in a minority of patients (those who also had a significant asthma component to their COPD), after the TORCH study in 2007, ICS and salmeterol together are thought to be beneficial in most patients (decreased exacerbations and perhaps decreased mortality) |
|
|
Term
| SE of Inhaled Corticosteroids |
|
Definition
| Increase at high-dose: osteopenia, delayed growth in kids, candidiasis |
|
|
Term
| MOA of Systemic (PO or IV) Steroids |
|
Definition
| Anti-inflammatory Rx; will take hours before onset of action |
|
|
Term
| Examples of Systemic (PO or IV) Steroids |
|
Definition
| PO - usually prednisone; IV - usually methylprednisone (solumedrol) |
|
|
Term
| IND for Systemic (PO or IV) Steroids |
|
Definition
| In Asthma - for severe flares not responding to inhalers; In COPD - for severe, acute exacerbations |
|
|
Term
| SE of Systemic (PO or IV) Steroids |
|
Definition
| More problematic than ICS; Cushingoid appearance, osteopenia, hyperglycemia, poor wound healing, increased susceptibility to infections |
|
|
Term
| Examples of Mast Cell Inhibitors |
|
Definition
| Cromolyn sodium (Intal), Nedocromil sodium (Tilade) |
|
|
Term
| MOA of Mast Cell Inhibitors |
|
Definition
| Take up to 4 wks to work; not a bronchodilator; mild anti-inflammatory effect; stabilizes mast cells |
|
|
Term
| IND for Mast Cell Inhibitors |
|
Definition
| For mild asthma when you want VERY safe Rx (kids, pregnant women); can block allergen-induced asthma if it's used before exposure to the allergen |
|
|
Term
| SE of Mast Cell Inhibitors |
|
Definition
| Since it's poorly absorbed, no systemic problems; minor local effects |
|
|
Term
|
Definition
| Leukotrienes are potent bronchoconstrictors and asthmatic patients are more sensitive to their bronchoconstricting effects. Antileukotrienes either prevent the synthesis of leukotrienes (zileuton) or the attachment of leukotrienes to the receptor site (montelukast) - as of 2005 zileuton is off the market. |
|
|
Term
|
Definition
| For asthma, but not yet for monotherapy. ICS are preferred over antileukotrienes for initial Rx of persistenet asthma. May be useful in those on high-dose ICS when it's hard to get them down to low-dose regimens; useful in patients with ASA-induced asthma, prominent exercise-induced asthma. Approved for use in allergic rhinitis, but nasal steroids are preferred. |
|
|
Term
|
Definition
| Hepatotoxicity; drug-drug interactions; expensive, costing $75/ month |
|
|
Term
|
Definition
| AKA: Singulaire; of the Antileukotrienes available, this one seems the safest - it doesn't have hepatotoxicity or drug-drug interactions. May be safe to use in pregnancy, but use carefully and with expert advice |
|
|
Term
|
Definition
| Considered a drug; expensive to use chronically; IND - in selected end-stage COPD patients with chronic hypoxemia (usu. defined as a PaO2 <55mmHg on room air); Use in patients increases their quality of life and decreases mortality. |
|
|
Term
|
Definition
| Seldom needed or used by PCPs; oral long-acting preps are available |
|
|
Term
|
Definition
| IV Formulation; rarely used; this agent and theophylline have too narrow a "toxic-therapeutic ratio," side-effects include: nausea/ vomiting, drug-drug interactions, iregular HR and/or tachycardia; occassionally used by pulmonologists. |
|
|
Term
| Examples of Drugs for Smoking Cessation |
|
Definition
| Nicotine Replacement Therapy (NRT): OTC - nicotine gum, patches, lozenges; RX - nicotine spray, nicotine inhaler; Non-NRT: Buproprion (Zyban), Varenicline (chantix), Nortriptyline (seldom used, too many SE) |
|
|
Term
|
Definition
| MOA - not well understood; SE - avoid in patients with a history of or at risk for seizures; drug-drug interactions |
|
|
Term
|
Definition
| AKA - Chantix; MOA - partial agonist that binds selectively to nicotine acetylcholine receptors; SE - dose-dependent nausea, slight weight gain; Recent warning - the FDA has warned of neuropsychiatric sxs and exacerbations of pre-existing psychiatric illness (agitation, mood changes, suicidal ideation and behavior) |
|
|
Term
| Pharmacotherapy for Allergic Rhinitis |
|
Definition
| Antihistamines (1st and 2nd generation), Topical Intranasal Corticosteroids, Antileukotrienes, Cromolyn-nasal prep (Nasalcrom) |
|
|
Term
| Prototype 1st Generation Antihistamine |
|
Definition
| diphenhydramine (Benadryl) |
|
|
Term
| MOA of 1st Generation Antihistamines |
|
Definition
| Non-selective H1 (histamine) receptor antagonists. They're lipophilic, so they can cross the blood-brain barrier, increasing CNS side-effects |
|
|
Term
| IND for 1st Generation Antihistamines |
|
Definition
| Effective and inexpensive antihistamines, but usually with too many side-effects |
|
|
Term
| SE of 1st Generation Antihistamines |
|
Definition
| Sedation, decreased cognitive ability (affecting school children, drivers, etc.) |
|
|
Term
| MOA of 2nd Generation Antihistamines |
|
Definition
| So-called "selective H1-receptor antagonists." Less lipophilic than 1st generation agents, so there's less CNS penetration - fewer side-effects |
|
|
Term
| IND for 2nd Generation Antihistamines |
|
Definition
| Useful when patient needs occassional/ episodic control of allergic rhinitis without the SE of 1st generation agents |
|
|
Term
| OTC 2nd Generation Antihistamines |
|
Definition
| Loratadine, Claritin Reditabs, Alavert |
|
|
Term
| Rx Preps of 2nd Generation Antihistamines |
|
Definition
| Cetirizine (I believe you can buy this OTC now, but Dr. Reese lists it as Rx), fexofenadine (allegra), desloratadine (Clarinex) -- Fexofenadine is the preferred agent |
|
|
Term
| MOA of Topical Intranasal Corticosteroids |
|
Definition
| Reduces nasal eosinophilia, mast cells and cytokine expression, but takes several days to reach maximum efficacy |
|
|
Term
| IND for Topical Intranasal Corticosteroids |
|
Definition
| Optimal drug for control of sustained allergic rhinitis sxs, avoids drowsiness |
|
|
Term
| Examples of Topical Intranasal Corticosteroids |
|
Definition
| Beclomethasone (Beconase, Vancenase), and Fluticasone (Flonase) |
|
|
Term
| MOA of Cromolyn Nasal Prep |
|
Definition
| Stabilizes mast cells; Note - this is a different formulation than the cromolyn inhaler used for asthma, and the use of the inhaler for asthma requires a Rx |
|
|
Term
| IND for Cromolyn Nasal Prep |
|
Definition
| May work for MILD cases of allergic rhinitis; for moderate cases, topical nasal steroids work better and are preferred |
|
|
Term
| SE of Cromolyn Nasal Prep |
|
Definition
| No systemic problems since it's not absorbed |
|
|
Term
| Special Use Pulmonary Agents |
|
Definition
| Dornase-alpha (AKA - Pulmozyme; used for Cystic Fibrosis), Prostacyclin (AKA epoprostenol; used for Primary Pulmonary HTN) |
|
|
Term
|
Definition
| A recombinant human DNAse; An enzyme that hydrolyzes extracellular DNA; in CF patients, their sputum is more viscous than normal, in part because it contains large quantities of DNA released from disintegrated neutrophils. Normally, the pancreas makes small amounts of DNAse, but the pancreas in CF patients isn't normal |
|
|
Term
|
Definition
| Used in CF patients to decrease sputum viscosity, improve pulmonary function and decrease pulmonary infections; once a day or twice a day via nebulizer over 10 minutes |
|
|
Term
|
Definition
| Pharyngitis, laryngitis, voice alteration, expensive (>$10,000/yr) |
|
|
Term
|
Definition
| A potent vasodilator; how it decreases pulmonary vascular resistance remains unclear (it's not just vasodilation, remodelling occurs) |
|
|
Term
|
Definition
| Used to treat primary pulmonary HTN; continuous IV adminstration; has a few limitations - limited supply, VERY expensive |
|
|
Term
|
Definition
| Nausea, anorexia, jaw pain, complications of central venous catheter administration |
|
|
Term
| Antibiotics used for URIs |
|
Definition
| Penicillin, erythromycin, azithromycin; 2nd and 3rd generation cephalosporins (ex: ceftriaxone, cefepine); "Respiratory quinolones" (ex: levofloxacin, gatifloxacin, moxfloxacin); Piperacillin-tazobactam (Zosyn); Aminoglycosides (gentamycin or tobramycin for Hospital Acquired Pneumonia) |
|
|
Term
|
Definition
| Cidal - kills the TB organism; INH can inhibit the synthesis of cell wall components (mycolic acid) |
|
|
Term
| Pharmacokinetics/ Pharmacodynamics of Isoniazid |
|
Definition
| Typically given PO (300mg qd); good CNS penetration; metabolized by the liver (INH will decrease clearance of phenytoin) |
|
|
Term
|
Definition
| HEPATITIS, peripheral neuropathy, hypersensitivity rxns |
|
|
Term
|
Definition
| Interferes with DNA synthesis of TB Bacteria (RIF binds to the DNA-dependent RNA polymerase, this prevents the enzyme from bindig to DNA and thereby prevents subsequent DNA transcription) |
|
|
Term
| Pharmacokinetics/ Pharmacodynamics of Rifampin |
|
Definition
| PO usually (IV only if the patient is NPO); excreted thru the liver via bile; good penetration including CNS; induces increased hepatic excretion of many drugs (oral contraceptives, warfarin, etc.) |
|
|
Term
|
Definition
| Hepatitis, body-fluid discoloration (red-orange), drug-drug interactions |
|
|
Term
|
Definition
| Interferes with cell wall synthesis; may allow other drugs (eg RIF) to cross the cell wall; "static" - inhibits growth, but doesn't kill the organism |
|
|
Term
| Pharmacokinetics/ Pharmacodynamics of Ethambutal |
|
Definition
| PO; 50% excretion by kidneys; poor CNS penetration |
|
|
Term
|
Definition
| Optic neuritis (patients need serial eye clinic checks), hyperuricemia |
|
|
Term
| MOA of Pyrazinamide (PZA) |
|
Definition
| Not really understood; since it's converted to pyrazinoic acid, it may lower the pH; works intracellularly; cidal |
|
|
Term
| Pharmacokinetics/ Pharmacodynamics of of Pyrazinamide |
|
Definition
| PO; penetrates inflammed CNS |
|
|
Term
|
Definition
|
|
Term
|
Definition
| An inhibitor of protein synthesis; cidal; An aminoglycoside |
|
|
Term
| Pharmacokinetics/ Pharmacodynamics of Streptomycin |
|
Definition
| Only IM; fair penetration of inflamed CNS; renally excreted |
|
|
Term
|
Definition
|
|
Term
|
Definition
| Drugs that Increase DA levels: Carbidopa/ Levodopa (sinemet), Amantadine(Symmetrel); DA Receptor Agonists: Pramipexole(Mirapex), Ropinirole (Requip); COMT Inhibitors: Entacapone (Comtan); Anticholinergic Drugs: Trihexyphenidyl (Artane) |
|
|
Term
|
Definition
AKA Sinemet; MOA - Carbidopa inhibits the decarboxylation of peripheral levodopa, it doesn't cross the BBB. Levodopa, in the presence of carbidopa, crosses the BBB and is decarboxylated into DA;
Other - with chronic use, up to 75% of patients develop motor complications including drug-induced dyskinesias and on-off motor fluctuations (rapid changes from good to poor response) - consequently, many doctors don't use carbidopa/levodopa early in disease, especially in younger patients. However, in the older patient it is often the DOC |
|
|
Term
|
Definition
| AKA Symmetrel; MOA - Releases DA from intact dopaminergic terminals that remain in the SN; You may see this used for early, mild PD and L-dopa dyskinesias; In older patients, it may cause too many side-effects including confusion and swollen ankles, so its use is typically limited to younger patients; Also has muscarinic effects |
|
|
Term
|
Definition
| AKA Mirapex; MOA - direct stimulation of DA receptors; overall this has less efficacy and more short-term side effects than L-dopa; some feel younger patients (<65) are better candidates for DA agonists in hopes of avoiding long-term L-dopa use complications; used with L-dopa in advanced disease; SE - postural hypotension, hallucinations, drowsiness |
|
|
Term
|
Definition
| AKA Requip; Works the same was as pramipexole |
|
|
Term
|
Definition
| AKA Comtan; MOA - Inhibits the metabolism of DA, thereby increasing levels of DA; COMT (Catechol-O-methyltransferase) is the enzyme that breaks down L-dopa, so COMT inhibitors are given with L-dopa to prolong its half-life; SE - GI (nausea, diarrhea), dyskinesias, and urine discoloration; Tolcopone (Tasmar) is a related drug, but it's not used in Canada or much in the US because it causes hepatotoxicity |
|
|
Term
|
Definition
| AKA Artane; MOA - inhibits muscarinic cholinergic CNS receptors (in PD, the loss of DA neurons leads to increased firing of cholinergic neurons with overstimulation of muscarinic receptors); Effective in treating tremor; typically restricted to young patients with mild disease |
|
|
Term
|
Definition
| MOA - block sodium channels, preventing generation and conduction of n. impulses; IND - used for local anesthesia (ex: dental extraction, suturing); Examples - lidocaine (xylocaine), Procaine (novocaine), Bupivacaine (Marcaine), Cocaine; Two types - Amides and esters - amides have an "i" in the part of the name that preceds the "-caine" part (ex: bupivacaine, lidocaine), esters do not (ex: cocaine, procaine) |
|
|
Term
|
Definition
| AKA Novocaine; The prototypical ester-type local anesthetic; Effective action is transient; Used for infiltration anesthesia |
|
|
Term
|
Definition
| A long-acting, more potent ester-type local anesthetic than procaine; widely used for topical and spinal anesthesia |
|
|
Term
|
Definition
| Short-acting ester-type local anesthetic; useful in some surgical and OB procedures; Low toxicity |
|
|
Term
|
Definition
| An ester-type local anesthetic; Useful in prolonged surface anesthesia due to its very low solubility in H2O |
|
|
Term
|
Definition
| The most widely used local anesthetic; Can be used for infiltration, spinal and surface anesthesia; Has some vasoconstrictive properties and can be used with or without added vasoconstrictive agents |
|
|
Term
|
Definition
| An amide-type local anesthetic with similar properties to Lidocaine with a more rapid onset of action and a more prolonged effect |
|
|
Term
|
Definition
| An amide-type local anesthetic; A potent injectible agent with a long duration of action |
|
|
Term
|
Definition
| Act as agonists at the mu, delta and kappa opioid receptors; work primarily through Gi/Go proteins to hyperpolarize neurons and inhibit neurotransmitter release |
|
|
Term
|
Definition
| Relief of moderate to severe pain, pre-op medication and as adjuncts during anesthesia. Some agents (eg codeine) are used for their antitussive effects and others for their antidiarrheal effects |
|
|
Term
|
Definition
|
|
Term
|
Definition
| Usually characterized by coma with marked respiratory depression and pinpoint pupils (miosis). Hypotension and decreased bowel sounds are also commonly observed. The diagnosis can be confirmed by giving naloxone (Narcan), a general opioid antagonist. Note - severe withdrawal can be caused by naloxone in a physically dependent patient |
|
|
Term
| Synthetic Opioid Agonists |
|
Definition
| Fentanyl (Duragesic), Meperidine (Demerol), Propoxyphene/ Acetominophine (Darvocet), Tramadol (Ultram), Methadone (Dolophine), Remifentanil (Ultiva) |
|
|
Term
| Opioid-Related Compounds Used as Antidiarrheal Agents |
|
Definition
| Diphenoxylate (Lomotil), Loperamide (Imodium) |
|
|
Term
| Partial Opioid Agonists and Mixed Agonists/ Antagonists |
|
Definition
| Buprenorphine (Buprinex), Nalbuphine (Nubain); Mixed opioid agonists/ antagonists are characterized by different actions on each of the opioid receptors: nalbuphine - kappa agonist/ mu antagonist, buprenorphine - partial mu agonist, pentazocine - kappa agonist, weak mu agonist; these agents are contraindicated in opioid dependent patients as severe withdrawal syndrome may develop |
|
|
Term
| Synthetic Opioid Antagonists |
|
Definition
| Naloxone (Narcan) - MOA: displaces opioid narcotics from receptor sites, IND: reverses CNS and respiratory depression in suspected overdose; Naltrexone (Revia) - longer acting bioavailable opioid antagonist used for treatment of opioid addiction and alcoholism |
|
|
Term
| Opioid Agonists related to Morphine/ Codeine |
|
Definition
| Morphine (MS Contin, MSIR); Codeine/ Acetominophen (Tylenol #3); Hydrocodone/ Acetominophen (Vicodin); Oxycodone, Oxycodone/ Acetominophen (Oxycontin, Percocet); Heroin |
|
|
Term
|
Definition
| The prototypical mu opioid agonist; Indicated for moderate to severe pain; Multiple preparations available - parenteral, oral and sustained release (MS Contin), rectal; M3B and M6B glucoronides are primary metabolites - may contribute to analgesic effects (M6B) and side-effects (M3B); Lower dosing in geriatric patients (smaller Vd and decreased renal function); Morphine produces histamine release - bronchoconstriction and vasodilation; patients with decreased blood volume are more sensitive to the vasodilatory effects of morphine |
|
|
Term
|
Definition
| A weak opioid analgesic; Has limited affinity for opioid receptors; Considered a prodrug - Needs to be demethylated to morphine; Approximately 10% of Caucasians lack the CYP540 isozyme to do this - these patients will get no relief from even high doses of codeine |
|
|
Term
|
Definition
| Full opioid agonist; Similar efficacy to morphine; Good oral bioavailability; Long half-life and duration of action; The compound has antagonist actions at the NMDA receptor complex - leads to decreased development of tolerance and physical dependence? role in treatment of neuropathic pain?; Used in treatment of heroin addiction and managing opioid withdrawal |
|
|
Term
|
Definition
| Relatively selective mu opioid agonists; Typically more potent than morphine; Shorter duration of action (eg remifentanil); High efficacy; Fentanyl can be given by various routes - transdermal patch, fentanyl lozenge (lollipop); Muscular rigidity more prolonged with this class of compounds compared to morphine |
|
|
Term
|
Definition
| AKA Demerol; Moderate efficacy opioid agonist; Used for moderate pain; The compound has antimuscarinic effects, cardiovascular effects are possible; Causes limited constriction of the pupil; Accumulation of normeperidine can produce seizures; Caution with high doses and in patients with renal insufficiency; No longer recommended for management of chronic paine; Don't use with MAOIs (Serotonin Syndrome); Other - applications in labor and delivery?, decreased urinary retention vs. morphine?, used to treat post-anesthetic shivering |
|
|
Term
|
Definition
| Opioid agonist with moderate efficacy; Recent controversy with this drug; Sustained release prep (oxycontin); Pellets can be crushed and a solution injected; Purdue Pharma has tried to reformulate the compound with naloxone so that oral administration would still be effective, but parenteral administration would result in blockade of opioid actions |
|
|
Term
|
Definition
| Very weak opioid agonist; Analgesic effect equivalent to aspirin when used alone; Typically administered in combination with aspirin (ASA) and acetominophen (APAP); Limited clinical utility; Concern with accumulation of norpropoxyphene (convulsions, hallucinations and cardiotoxicity are possible); Irritating to tissue when injected |
|
|
Term
| Diphenoxylate/ Loperamide |
|
Definition
| Diphenoxylate is a weak opioid agonist with low abuse liability, atropine is added as a combination product for treatment of diarrhea and to discourage abuse; Loperamide is a moderate efficacy opioid agonist that doesn't readily cross the BBB, low abuse liability, common OTC anti-diarrheal medication |
|
|
Term
|
Definition
| AKA Ultram; Novel analgesic action; Weak mu opioid agonist; Blocks reuptake of Serotonin (5HT) and norepinephrine; Marketed as a compound with efficacy similar to codeine with less side-effects; No addiction liability?; Less GI effects; Efficacy in neuropathic pain states; Expensive |
|
|
Term
|
Definition
| AKA Narcan; Prototypical opioid antagonist; Used to treat opioid overdoses; Low oral bioavailability; Short duration of action; Will precipitate a severe withdrawal syndrome in opioid dependent patients; New evidence suggests that this compound has inverse agonist actions in opioid-dependent states |
|
|
Term
|
Definition
| Prototypical opioid antagonist; Used to treat heroin addicts; Good oral bioavailability; Long duration of action; New evidence suggests that this compound has inverse agonist actions in opioid-dependent states; role in patient compliance?; Approved for the treatment of alcoholism - decreases binge-type drinking |
|
|
Term
|
Definition
| First in class peripheral opioid antagonist - it has a quaternary nitrogen that prevents it from crossing the BBB; Must be given subcutaneously; Indicated for opioid-induced constipation in patients with advanced illness and who are not responding to conventional laxative treatment; Can produce severe diarrhea and abdominal cramping, especially in opioid-dependent patients; Contraindication of mechanical bowel obstruction |
|
|
Term
|
Definition
| Carbamazepine OR Lamotrigine OR Oxcarbazepine OR Levetiracetam |
|
|
Term
| DOC for Atypical absence, Myoclonic and Atonic Seizures |
|
Definition
| Valproate OR Lamotrigine OR Levetiracetam |
|
|
Term
| DOC for Generalized Tonic-Clonic (Grand Mal) Seizures |
|
Definition
| Valproate OR Lamotrigine OR Levetiracetam |
|
|
Term
| DOC for Absence (Petit Mal) Seizures |
|
Definition
| Ethosuximide OR Valproate |
|
|
Term
| Second-Line Anticonvulsant Agents |
|
Definition
| Phenytoin (Dilantin), Gabapentin (Neurontin), Topiramate (Topamax), Diazepam |
|
|
Term
|
Definition
| AKA - Dilantin; MOA - largely unknown, but may block sodium channels, thereby stabilizing the threshold against hyperexcitability, also blocks calcium channels and may enhance GABA; IND - not really considered a DOC anymore because of its complicated pharmacokinetics, inferior adverse event profile and frequent drug-drug interactions; SE - nystagmus (even at therapeutic concentrations), drowsiness, ataxia and diplopia, rash and other hypersensitivity reactions, gingival hyperplasia |
|
|
Term
|
Definition
| AKA- Neurontin; IND - combination Rx, also used for chronic pain syndromes; Few drug-drug interactions |
|
|
Term
|
Definition
| AKA - Topamax; IND - adjunctive Rx for many seizure types, also used as a prophylactic agent for migranes and treatment of neuropathic pain; SE - paresthesias, cognitive impairment, it's a weak carbonic anhydrase inhibitor, and if used chronically may cause a metabilic acidosis which can increase the risk of renal calculi |
|
|
Term
|
Definition
| The rectal gel formulation (Diastat/ AcuDial) is approved for Rx of repetitive seizures; Delivered this way, diazepam is rapidly and completely absorbed and effective in treating acute repetitive seizures; It's approved for intermittent use in Rx-increased seizure activity in patients taking other antiepileptic drugs; May decrease the need for ER visits; Comes in single-dose pre-filled syringes as well |
|
|
Term
|
Definition
| AKA - Tegretol; DOC - partial seizures; MOA - appears to act by reducing polysynaptic responses and blocking post-tetanic potentiation, also used to treat the chronic pain of trigeminal neuralgia and diabetic neuropathy; SE - Rash, Asian patients are at risk for severe skin rahses (stevens-johnson syndrome) based on genetic predisposition (HLA-B15o2) which can be tested for in advance, CNS sxs (drowsiness, HA, decreased cognitive function) may increase in patients with absence seizures; Mild leukopenia, hyponatremia; MANY drug-drug interactions - look them up for each patient |
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Term
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Definition
| AKA- Trileptal; IND - for partial seizures; Similar MOA and SE to carbamazepine |
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Term
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Definition
| AKA - Zarontin; DOC - Absence (petit mal) seizures; SE - usually well tolerated, GI - nausea/ vomiting, hiccups |
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Term
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Definition
| AKA - Valproic acid (generic) or Depakote (trade name); DOC - for Grand Mal, Petit Mal, Atypical Absence, Myoclonic and Atonic seizures; MOA - may increase brain levels of GABA, also used as a mood stabilizer; SE - nausea/ vomiting are the most common - can be decreased with enteric coating, taking with food, weight gain is fairly common, unexplained hepatotoxicity has occurred (especially when used in <2 y/o patients) - so monitor LFTs; Decreases the clearance of Lamotrigine |
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Term
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Definition
| AKA - Keppra; DOC - Grand Mal, partial, atypical absence, myoclonic and atonic seizures; IND - FDA approved for adjunctive treatment, oral and IV forms are available, approved for adults and kids >4 with partial seizures, adults and kids >6 with primary generalized seizures, adults and kids >12 with myoclonic seizures; MOA - binds selectively to the synaptic vesicular protein SV2A, which may modify the synaptic release of glutamate and GABA; SE - Somnolence, dizziness, weakness and irritability, but no life-threatening SE; Few drug-drug interactions because it's not metabolized by the CYP450 system |
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Term
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Definition
| AKA - Lamictal; DOC - grand mal, partial, atypical absence, myoclonic and atonic seizures; IND - used as monotherapy in some adults and adjunctive therapy in adults and kids >2; Decrease dose and rate of dose increase when used with valproate (because valproate decreases the clearance of lamotrigine); SE - rash, may be diffuse and severe with a Stevens- Johnson Syndrome |
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Term
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Definition
| AKA - Desyrel; Has a sedating effect and may be used as an adjunct for SSRI-induced sleep disturbances; May cause orthostatic hypotension when first started and this may increase the risk of falls when used in the elderly; Priapism - seen on Boards, but is clinically rare |
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Term
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Definition
| AKA - Clozaril; An atypical antipsychotic agent; Has been around a long time and may be the most effective agent; Its routine use is limited since it causes granulocytopenia or agranulocytosis in about 1% of patients; Still used in patients not responding to other drugs; Intially, weekly or even twice weekly blood counts are MANDATORY to monitor the WBC count. If the WBC count remains stable on Rx for about 6 months, blood counts may then be done every other week |
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Term
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Definition
| AKA - Wellbutrin; MOA - not fully understood; Used as both an antidepressant and as a stop-smoking aid (Zyban); Doesn't seem to cause weight gain, sexual dysfunction or sedation - so it may be useful in patients who can't tolerate other antidepressants; May be useful in patients with erectile dysfunction from SSRIs; Useful in combination Rx to augment another antidepressant; Avoid in patients with a history of seizures or eating disorders |
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Term
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Definition
| AKA - Cymbalta; A new SSRI; Also approved for treatment of neuropathic pain and is marketed particularly for Rx of depression in patients with prominent pain complaints |
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Term
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Definition
| AKA - MPH; This is the active incredient in the majority of stimulant meds prescribed in the US and is effective in adults and kids; MOA - MPH is thought to block reuptake of DA into presynaptic neurons in the CNS, increasing the concentration in the interneuronal space; Short-acting preps: ritalin, methylin; Intermediate-acting preps: ritalin SR (sustained release), methylin ER; Long-acting Preps: Ritalin LA |
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Term
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Definition
| AKA - Eskalith, Litholoid; MOA - alters sodium transport in nerves and muscle cells; Its antimanic effects may be the result of increased reuptake of norepinephrine; IND - a mood stabilizer used to treat bipolar disorder; SE - the toxicity of lithium is closely related to serum lithium levels and can occur at therapeutic doses, therefore, serum lithium levels are required to monitor treatment (the level should be between 0.8-1.3); Signs of toxicity include - tremor, ataxia and changes in mental status (eg confusion); Must also monitor renal function and thyroid function (hypothyroidism is a concern) |
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Term
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Definition
| AKA - Tegretol; Has been used to treat mania and may be helpful for patients intolerant of, or nonresponsive to, lithium or valproate (but isn't as commonly used as either of them) |
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Term
|
Definition
| AKA - Effecor; MOA - a potent inhibitor of the reuptake of both serotonin and norepinephrine; Might be more effective than an SSRI for some patients with depression, but for the majority of patients, SSRIs appear just as effective; May be useful in neuropathic pain |
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Term
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Definition
| Available either as the d-isomer or in racemic forms, which are mixtures of d- and l-amphetamines; Dextroamphetamine (eg Dexedrine - short and long acting preps) -a d-isomer; Adderall is a mixture of amphetamine salts; There's no evidence that mixed amphetamine salts offer any advantages over methylphenidate (MPH) or dextroamphetamine, but some patients respond to one and not the other; SE - delayed sleep onset, HA, decreased appetite and weight loss; SE leading to discontinuation of Rx include - motor and vocal tics, anorexia, tachycardia and insomnia; Drug-drug interactions have been described |
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Term
| Tricyclic Antidepressants |
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Definition
| MOA - Block reuptake of both norepinephrine and serotonin; SE - anticholinergic (urinary retention, constipation, dry mouth, etc.), sedative, sexual dysfunction and orthostatic hypotension; Because of these SE, they're not used as much anymore; Cardiotoxic in overdose; IND - patients who can't afford newer meds, patients who benefit from the SE (ex: depression with insomnia would benefit from sedation); Note - serum levels can be obtained; Ex - Amytriptyline (Elavil), desipramine (Norpramin), nortriptyline (Pamelor) |
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Term
| Cholinesterase Inhibitors |
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Definition
| MOA - centrally acting cholinesterase inhibition; IND - treatment of mild to moderate Alzheimers ds; Ex - donepezil (Aricept), rivastigmine (Exelon), tacrine (Cognex) |
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Term
|
Definition
| MOA - addictive properties are thought to be due to the release of DA in the limbic forebrain regions; EtOH; Stimulants (amphetamine, cocaine, methamphetamine); Opioids (morphine, heroin); Hallucinogens (LSD, MDMA/ Ecstasy, phencyclidine/ PCP, ketamine); Marijuana |
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Term
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Definition
| Methadone, Naltrexone (ReVia), Buprenorphine, Acamprosate (Campral) |
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Term
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Definition
| AKA - Campral; An oral medication taken 3x/day; Rx should be part of a comprehensive treatment program which includes psychosocial support; IND - to maintain abstinence from EtOH; MOA - structurally resembles GABA, so acamprosate decreases glutamatergic transmission and modulates neuronal excitability during withdrawal from EtOH; SE - generally safe, diarrhea is the most common SE, appears dose-related, suicidal ideation and acute renal failure have occurred |
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Term
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Definition
| AKA- Ambien; A non-benzodiazepine used as a hypnotic; Binds to specific benzodiazepine receptors; Long-acting CR formulations are now available; May cause dream-like states during the day; Rx has been associated with MVAs; May have abuse potential, especially at high doses; Zeleplon (Sonata) and eszopiclone (Lunesta) have similar indications and efficacy |
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Term
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Definition
| AKA - Buspar; A non-benzodiazepine antianxiety drug which is non-sedating and non-addicting, but may take up to 4 weeks to act and may be less effective than antidepressants or benzos for anxiety; Usually not effective in low doses; Don't Rx it for major depression or panic attacks as it is inadequate therapy |
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Term
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Definition
| AKA - Valproate, Depakote; May be as effective as lithium for the treatment of mania; In particular, the divalproex formation of valproic acid; Depakote levels should be between 95-150 |
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Term
| Drugs for Bipolar Disorder |
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Definition
| Mood stabilizers; Lithium, valproic acid, carbamazepine, lamotrigine |
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Term
| Drugs for ADD with or without Hyperactivity |
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Definition
| Stimulants - methylphenidate (MPH), amphetamines; Non-stimulants - atomoxetine (Strattera) |
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Term
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Definition
| MOA - depresses sensory cortex, decreases motor activity, alters cerebellar function and produces drowsiness, sedation and hypnosis by facilitation of GABA activity thru increasing chloride channel opening; Overdose can lead to respiratory depression or coma; These drugs are rarely used in psych now and are often viewed as 3rd-line drugs because of the SE; IND - used as sedatives, hypnotics and occassionally as anticonvulsants; EX - phenobarbitol (Luminal) |
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Term
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Definition
| Bind to the benzodiazepine receptors, potentiating the effect of the inhibitory neurotransmitter GABA by increasing the frequency of chloride channel opening, which leads to decreased neuronal firing |
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Term
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Definition
| Used to treat anxiety and as sedatives, hypnotics, anticonvulsants and muscle relaxants. (Medical Letter suggests using an anti-depressant - usually a SSRI - as the DOC in anxiety treatment); Benzos are potentially addicting and have limited benefit in OCD or PTSD; Generally recmmoneded for short-term or intermittent use |
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Term
| Examples of Benzodiazepines |
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Definition
| NOTE: Drugs in this category all end in "pam" or "lam"; Alprazolam (Xanax) - high abuse potential due to short half-life; Clonazepam (Klonopin) - less abuse potential, more sedating, helpful with sleep, often used in mania; Diazepam (Valium) - "outdated," often abused, long half-life, may be helpful in EtOH withdrawal and DTs; Lorazepam (Ativan) - commonly used for anxiety, intermediate half-life, often used in patients with respiratory and cardiac dysfunction in palliative care; Midazolam (Versed) - used mostly as an induction agent for procedures |
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Term
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Definition
| Somnolence; Interference with psychomotor performance; Impaired memory; Addiction potential (increased in those with a predisposition to drug/ alcohol abuse); Because of these SE, the benzos are for acute sxs of anxiety and panic attacks, SSRIs are preferred for long-term Rx |
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Term
| MOA of Atypical Antipsychotics |
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Definition
| AKA - 2nd Generation Antipsychotic agents; MOA - Antagonists at both the DA (D2 and D4) and Serotonin Receptor (5HT2) as well as other receptors |
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Term
| IND for Atypical Antipsychotics |
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Definition
| Preferred over typical antipsychotics because they're safer, adherence is better and the risk of tardive dyskinesia is lower; May still cause neuroleptic malignant syndrome (NMS); Used for schizophrenia, psychosis and may be used for chronic aggression and bipolar disorders |
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Term
| SE of Atypical Antipsychotics |
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Definition
| Elderly people may have a higher mortality rate than those on placebos; Implicated in "metabolic syndrome" with obesity, hyperglycemia and hyperlipidemia - hyperglycemia especially can occur with these atypical agents |
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Term
| Examples of Atypical Antipsychotics |
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Definition
| Quetiapine (Seroquel) - also used for patients with Parkinson's and Lewy Body Dementia, also being used in the Rx of anxiety and insomnia by PCPs; Olanzapine (Zyprexa); Risperidone (Resperdal); Dozapine (Clozaril); Ziprasidone (Geodon); Aripiprazole (Abilify) |
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Term
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Definition
| AKA - 1st generation antipsychotics; MOA - antagonists at the DA receptor (D2>D1); IND - used to treat schizophrenia and psychosis (also used in bipolar disorder and aggression); SE - anticholinergic, sedative, sexual dysfunction and orthostatic hypotension, no cardiotoxicity, have the ability to induce extrapyramidal side effects including tardive dyskinesias and neuroleptic malignant syndrome (NMS) which is uncommon; Examples - haloperidol (Haldol), also used to treat Tourette's and Huntington's; Thioridazine (Mellaril); Chlorpromazine (Thorazine) |
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Term
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Definition
| AKA - Strattera; MOA - it is a selective norepinephrine reuptake inhibitor; SE - somnolence, nausea/ vomiting; Not as well tolerated or effective as Methylphenidate (MPH) and is best reserved for patients who haven't responded to or cannot take stimulants |
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Term
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Definition
| MOA - selectively inhibit the reuptake of serotonin (5HT); SE - few side effects compared to TCAs and less toxic in overdose, side-effects include - transient Headaches, GI sxs, sweating and sexual dysfunction; Note - also DOC for panic disorder and OCD (may need higher doses), commonly used in social anxiety disorder and PTSD |
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Term
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Definition
| Fluoxetine (Prozac), Paroxetine (Paxil), Sertraline (Zoloft), Citalopram (Celexa), Escitalopram (Lexapro), Fluoxamine (Luvox) |
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Term
| SSRI Treatment in Children |
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Definition
| Fluoxetine (Prozac) is the only SSRI approved by the FDA for Rx of major depressive dissorder in children and adolescents; "Black Box" warnings are now on all antidepressant drug labels because of concerns that SSRIs (and SNRIs) could cause depressed children/ adolescents to attempt suicide |
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Term
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Definition
| Can occur when SSRIs (or SNRIs) interact with MAOIs or drugs with MAOI activity such as the antibiotic Linezolid and some other serotonergic drugs such as dextromethorphan (anti-tussive), tramadol, sumatriptan and St. John's Wort; Patients with this syndrome have - fever, altered mental status, tachycardia, HTN, agitation, tremor, hyper-reflexia, etc. |
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Term
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Definition
| AKA - Geodon; The first atypical antipsychotic which is available in an IM form; Not a depot long-acting injection, but a rapid-onset injection marketed as being as effective as haloperidol for rapid sedation, but with less side effect potential; American Academy of ER Physicians now recommends Ziprasidone over haloperidol for Rx of acute agitation; A concern wtih the use of ziprasidone is the prolongation of the QT interval, so patients should have a baseline EKG before starting this medication; Should be taken with food to obtain optimal levels |
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Term
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Definition
| AKA - Abilify; A new agent; A D2 DA modulator and therefore a member of a new class of atypical antipsychotics; This drug and ziprasidone aren't considered potent agents and shouldn't be first line Rx for schizophrenia; Used to treat bipolar disorder/ mania in kids |
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Term
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Definition
| AKA - Risperdal; An atypical antipsychotic agent; There's a long-acting depot injection formulation which is expensive; Also comes in dissolvable formulations which are useful to treat patients that "cheek" their medications or when forced administration is required in psych or the ER; Used to treat bipolar disorder/ mania in kids |
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Term
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Definition
| AKA - Lamictal; Has been used for bipolar disorder; Requires a very slow initiation due to the risk of Stevens - Johnson Syndrome; May be helpful, especially in depressive episodes |
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Term
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Definition
| AKA - Dantrium; MOA - inhibits calcium release from the SR of skeletal muscle by limiting the ability of calcium and calmodulin to activate the RYR-1 ryanodine receptor in skeletal muscle; IND - Special use: Rx of malignant hyperthermia (rare), may be used to treat spasticity associated with spinal cord injury, stroke, CP, MS; SE - weakness, sedation, hepatotoxicity |
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Term
|
Definition
| AKA - Flexeril; MOA - believed to act centrally (in the brainstem) by interfering with polysynaptic reflexes (both gamma and alpha motor neurons and maybe even at the spinal cord) that maintain skeletal muscle tone. Ineffective in CP or spinal cord injury; Structurally related to the tricyclic antidepressants; Possible effects inlcude central and peripheral anticholinergic actions and a sedative effect; IND - used to manage acute painful MSK conditions associated with muscle spasm, off-label use to Rx fibromyalgia but little evidence of efficacy in this setting; SE - may cause dizziness, drowsiness, and confusion; dry mouth and other antimuscarinic effects; Additive effects with other CNS depressants |
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Term
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Definition
| MOA - bind/block/neutralize the activity of TNF alpha, an important cytokine in the pathogenesis of RA. May also be referred to as an anti-cytokine agent; Examples - Etanercept (Enbrel), Infliximab (Remicade), Adalimumab (Humira); Note - all of these agents are very expensive, costing >$11,000/ yr, though this must be weighed against the improved ability of some patients to work; SE - increased risk of infection (especially latent TB being "unmasked"), so check a baseline PPD and chest x-ray; Avoid use in patients with active/ chronic infection; Data suggest avoiding their use in patients with congestive heart failure or demyelinating disorders |
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Term
| IND for Etanercept (Enbrel) |
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Definition
| RA, Psoriasis, Juvenile RA, Psoriatic arthritis, Ankylosing Spondylitis |
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Term
| IND for Infliximab (Remicade) |
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Definition
| RA, Irritable Bowel Ds, Ankylosing Spondylitis, Psoriasis and psoriatic arthritis |
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Term
| IND for Adalimumab (Humira) |
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Definition
| RA, Ankylosing Spondylitis, Psoriatic arthritis, psoriasis, Chron's ds. |
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Term
| Agents Still Used in Early-Mild RA |
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Definition
Sulfasalazine (asulfidine) - less useful in moderately severe RA now with availability of newer agents, still used in joint disease associated with IBD and in seronegative spondyloarthropathies with peripheral joint involvement, SE - usually pretty well tolerated, mild GI upset is relatively common, leukopenia can occur so monitor CBC;
Hydroxychloroquine (Plaquenil) - may still be used in very mild RA, also used in cutaneous lupus, SE - usually pretty well tolerated except for mild GI sxs. There is a risk of retina toxicity with prolonged use, so proper dosing and periodic ophthalmologic exams (every 6-12 months) are advised, Photosensitivity can occur, so patients are advised to use sun screen |
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Term
| Neuromuscular Blocking Agents |
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Definition
Non-Depolarizing (Competitive nicotinic antagonists) - Pancuronium (Pavulon), Rocuronium (Zemuron, onset of action is quick: 1-2 min), Mivacurium (Mivacron);
Depolarizing (nicotinic agonist that leads to rapid receptor desensitization) - Succinylcholine (Anectine) |
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Term
|
Definition
| MOA - inhibition of inflammatory response; SE - systemic use is associated with increased risk of infection, cushingoid appearance, osteopenia with increased vertebral fractures, hyperglycemia, poor wound healing,etc.; Low-dose (eg 5mg/day) oral prednisone for RA; Intra-articular (eg triamcinolone hexacetamide) avoids systemic SE; high-doses of prednisone or methylprednisolone are occassionally used for RA vasculitis/ lupus nephritis |
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Term
| OTC "Non-Selective" or "Conventional Agent" NSAIDs |
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Definition
| MOA - reversible inhibition of COX1 and COX2; Low-dose regiments are on the packaging in hopes of decreasing GI side-effects; Ibuprofen (Motrin), Naproxen (Naprosyn); Other Conventional NSAIDs (once-daily, require Rx) - Piroxican (Feldene), Nabumetone (Relafen) |
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Term
|
Definition
| AKA - Toradol; An injectable NSAID; This agent is for short-term use (up to 5 days) to Rx moderately acute pain that typically requires analgesics at the opioid level; Not indicated for minor or chronic pain; The IV formulation may still be used for short periods in selected peri-operative settings; Prolonged use/ high doses can be associated with excessive SE (eg GI bleeding) |
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Term
| Selective COX2 Inhibitors |
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Definition
| These drugs have fewer GI SE than non-selective COX inhibitors (as long as the patient isn't on ASA); They're much more expensive than conventional or non-selective NSAIDs; Note that the COX2 selective agents are no more effective than non-selective agents; Celecoxib (Celebrex) is currently the only COX2 agent available; Rofecoxib (Vioxx) was withdrawn in 2004 over concerns of increased risk fo MI, Stroke, etc. |
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Term
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Definition
| MOA - Inhibits the migration of granulocytes; IV colchicine is no longer recommended (too many SE); Oral Rx used in limited situations - prophylaxis of acute flares of gout while treating someone's increased uric acid (with allopurinol for example); Colchicine is rarely favored in acute episodes of gout anymore, since there are better and less toxic drugs (ex NSAIDs - Indomethacin); Doses are adjusted in patients with renal failure |
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Term
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Definition
| AKA - Kineret; Less effective than TNF inhibitors; Used when other Rx won't work or can't be tolerated; May be good for juvenile RA, but it's an off-label use; MOA - an IL-1 receptor antagonist (remember - IL-1 is an important cytokine involved in the pathogenesis of RA); SE - headaches, injection site reactions, neutropenia and increased infections (especially if used with a TNF inhibitor) |
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Term
|
Definition
| AKA - Actemra; Was approved in mid-2008 for moderate-severe RA; Given IV every 4 weeks; MOA - the first IL-6 inhibitor; It is the first humanized IL-6 receptor inhibiting monoclonal antibody; SE - watch for elevated LFTs and lipid abnormalities |
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Term
|
Definition
| AKA - Cimiza; Approved in 2008 for Chron's disease; May play a role in RA Rx; MOA - pegolated TNF blocker with a long half-life |
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Term
|
Definition
| AKA - Tylenol; Still used for minor pain; It's also used as an anti-pyretic; It is NOT an anti-inflammatory or an anti-platelet agent; It has significant bleeding tendencies; MOA - Unclear, May act as a weak COX (3?) inhibitor; Centrally active without much effect on the peripheral tissue (so not a great anti-inflammatory agent for joints); SE - usually well tolerated if normal doses are followed (<3g/day in adults); Even with normal doses, mildly increased LFTs can occur and if this happens, the drug should probably be stopped; NOTE - many OTC preps contain APAP and if these are taken along with Tylenol or generic APA, excessive doses can be reached unintentionally; In excessive doses, esp. in patients with underlying liver disease, hepatotoxicity can occur and can be severe; Nephrotoxicity can occur with higher doses (>4g/day); GI ulcers and GI bleeding can occur (rare); Possible use of acetylcytesein (Mucomist) to neutralize toxic metabolites |
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Term
|
Definition
| Used for antipyretics, analgesia and/ or anti-inflammatory reasons; ASA, and other Conventional agents target COX1 and COX2 - some are reversible (Naproxen) while others are not (ASA); Selective agents target COX2 and their side effects may include increased risk of cardiovascular death; NSAID SE - although NSAIDs may cause edema and occassionally renal dysfunction and/ or HTN, the most common, worrisome SE is upper GI ulcers with GI bleeding, which can be life-threatening; Risk Factors associated with Increased Risk of GI Side-effects Include - age >60, history of ulcers, concomitant use of steroids or anticoagulants or ASA, high-dose or chronic use of NSAIDs and serious underlying disease |
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Term
|
Definition
| Used less for analgesia and/or anti-inflammatory agents since they cause too much GI toxicity in any chronic, full-dose regimens; Acetylated ASA (enteric-coated); Non-acetylated ASA - choline magnesium trisalicylate (Trilisate) |
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Term
|
Definition
| Colchicine, Allopurinol (Zyloprim), Indomethacine (Indocin), Probenecid |
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Term
|
Definition
| AKA - Zyloprim; Considered DOC for tophaceous gout and uric acid nephrolithiasis; MOA - inhibition of xanthine oxidase (prevents formation of uric acid); SE - diffuse rash, fever and increased LFTs |
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Term
|
Definition
| AKA - Indocin; An NSAID favored for acute attacks of gout |
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Term
|
Definition
| May still be used for uric acid "underexcretors" (Patiet has a low urine level of uric acid after a 24 hour urine collection); Not for acute Rx; MOA - this is a uricosuric drug, which lowers serum uric acid by blocking renal tubular reabsorption of urac acid; Use only in patients with a creatinine clearance of >50ml/min - so avoid in patients with renal failure, also avoid in patients with renal calculi; SE - GI upset, rashes; Encourage good fluid intake |
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Term
| Skeletal Muscle Relaxants |
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Definition
| Spasmolytics - diazepam (Valium), baclofen (Lioresal), tizanidine (Systemic), dantrolene (Dantrium), botulinum toxin A (Botox); Drugs for Acute Muscle Spasm due to Muscle Injury - cyclobenzaprine (Flexeril); Neuromuscular Blocking Agents - Non-depolarizing (competitive nicotinic antagonists), depolarizing (nicotinic agonist that leads to rapid receptor desensitization) |
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Term
|
Definition
| Diazepam (Valium), Tizanidine (Systemic), Dantrolene (Dantrium), and Botulinum Toxin A (Botox) |
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Term
|
Definition
| AKA - Valium; A benzodiazepine; IND - used to relieve m. spasms due to reflux spasm to local pathology (eg inflammation of muscles/ joints); Rx spasticity caused by upper motor neuron disorders; Rx anxiety for short term and Rx acute seizures including those related to EtOH withdrawal; MOA - facilitates the activity of GABA at the GABA-A Chloride channel (GABA is the major inhibitory neurotransmitter in the CNS); SE - sedation, drowsiness/ lethargy (especially in the elderly) |
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Term
|
Definition
| AKA - Lioresal; MOA - a GABA agonist, activates GABA-B receptors in the spinal cord; IND - used to Rx the spasticity associated with MS and other spinal cord injury/disease; Off-label use to Rx trigeminal neuralgia; PO or IV; SE - drowsiness, sedation, fatigue, but less so than with diazepam |
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Term
|
Definition
| MOA - clonidine-like effect: alpha-2 agonist, may decrease presynaptic release of excitatory transmitters; IND - used to decrease muscle tone and spasms (eg in MS); SE - dry mouth, drowsiness and at times hypotension |
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Term
|
Definition
| AKA - Botox; MOA- it is an enzyme which cleaves certain storage vesicle membrane proteins, blocking the release of acetylcholine from cholinergic nerver endings, causing a neuromuscular blocking effect; IND - Rx of certain focal dystonias and spasticity, also Rx of strabismus and blepharospasm associated with dystonia; SE - well tolerated when administered appropriately by experienced physicians, generalized muscle weakness (rare); Some patients develop antibodies to the toxin |
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Term
| Disease-Modifying Antirheumatic Drugs (DMARDs) |
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Definition
| Used to treat and prevent disease progression (ie joint damage) in RA especially; A rheumatologist usually directs their use because of their cost and/or toxicity and/or complexity of use/indications; Examples - methotrexate (MTX), TNF Inhibitors, Leflunomide (Arava), anakinra (Kineret); Other RA drugs - cyclophosphamide (Cytoxin), penicillamine (no longer used for RA), azathioprine (Imuran), cyclosporine, minocycline, gold, abatacept (Orencia), rituximab (Rituxan), sulfasalazine (Asulfidine), hydroxychloroquine (Plaquenil), tocilizumab (Actemra), certolizumab (Cimizia) |
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Term
|
Definition
| AKA - Rheumatrex; MOA - not entirely clear, MTX is an analog of folic acid and inhibits dihydrofolate reductase, impairing DNA synthesis (specifically purine synthesis) and decreases activated lymphocytes; IND - an important initial agent in moderate RA disease (and psoriatic arthritis); SE - GI upset, oral ulcers (stomatitis) and increased serum LFTs (so monitor LFTs); Also teratogenic and may cause lung abnormalities (eg pulmonary fibrosis which may look like a chronic pneumonia). Check a baseline chest x-ray and repeat if the patient develops pulmonary sxs. In practice, prefer to use if serum creatinine is <2; Serial CBCs are often done too |
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Term
|
Definition
| AKA - Arava; An immunosuppresive agent; MOA - leflunomide is the prodrug - it undergoes conversion to an active metabolite which inhibits dihydroorotate dehydrogenase, the rate-limiting intracellular enzyme which is required for pyrimidine nucleotide synthesis (so, in short, it's an inhibitor of pyrimidine synthesis); SE - Increased LFTs, so monitor them; teratogenic; long half-life (if a woman wants to get pregnant, you can increase its excretion by giving her cholestyramine which blocks its reabsorption). If leflunomide is combined with MTX, the risk of hepatotoxicity increases, so if leflunomide is added, start with lower doses of leflunomide |
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Term
| Agents Seldom Used for RA |
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Definition
| Clyclophosphamide (Cytoxan) - may also still use in Wegener's and severe vasculitis; Azathioprine (Imuran) - worry about malignancies after use, still may see use in severe systemic vasculitis; Penicillamine - no longer used in RA, too many SE; Cyclosporine - newer agents are more effective, this agent has many SE; Minocycline (Anabx) - used in the past for mild early RA, more studies needed; Gold - other agents much more effective, IM prep seldom used, oral not used |
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Term
| Other Agents for Refractory RA |
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Definition
Abatacept (Orancia) - an inhibitor of T-cell activation for moderate to severe RA not responding to traditional DMARDs (ie MTX or leflunomide), IV medication, Monthly cost is $1350/month, may cause serious infections, also used in selected cases of juvenile RA in kids >6;
Rituximab (Rituxan) - an anti-CD20 monoclonal antibody (depleats the CD20 Bcells, which apparently play a role in autoimmune process and synovitis of RA), to be used with MTX in refractory RA (those failing TNF inhibitors), Give 1 dose and repeat in 2 wks, given IV and very expensive (>$1300/dose), Next IV infusion is really as needed and at least at a 4 month interval (therefore you may see it given every 4-12 months), may cause infections, to decrease hypersensitivity reactions IV steroids may be given 30 min before; this agent is also used for B-cell non-Hodgkin's lymphoma |
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