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195 Cards in this Set
- Front
- Back
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Alprostadil
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Prostaglandin PGE1
- Vasodilation in tx of impotence - Maintain ductus arteriosus p/t surgery |
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Misoprostol
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Prostaglandin PGE1 derivative
- Used with mifepristone (RU486) in termination of pregnancy - Protection against peptic ulcer |
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PGE2 and PGF2alpha
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Prostaglandins
- Used with oxytocin to induce labor |
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Prostacyclin
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Prostaglandin
- Tx of pulmonary and portopulmonary HTN |
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Epoprostenol
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Prostaglandin - commercial preparation of PGI2
- Tx of pulmonary HTN - Very short t1/2 so requires IV |
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Iloprost
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Prostacyclin analog
- Inhalation 6-9 x daily |
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Latanoprost
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Stable long acting derivative of PGF2alpha
- First prostanoid used for glaucoma |
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Bimatoprost
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Prostanoids with hypotensive effects in the eye
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Travoprost
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Prostanoids with hypotensive effects in the eye
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Unoprostone
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Prostanoids with hypotensive effects in the eye
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Aspirin
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COX 1 and 2 inhibitor (higher affinity for COX 1)
Irreversible d/t acetylation of active site of both enzyme forms - Analgesia - PGs are moderators of nervous activity in PNS & CNS - Antipyresis - Blocks pyrogen induced PG synthesis to lower fever - Antiinflammation - reduces heat, pain and swelling - Antithrombotic - inhibits platelet COX 1 permenantly Overdose is common in kids -> central effects, vertigo, hyperventilation -> respiratory alkalosis -> metabolic acidosis -> CNS mediated hyperthermia and resp depression -> resp and vasomotor collapse Side effects: - Gastric Irritation, bleeding and ulcers - Precipitation of gout - Reyes syndrome in kids - exacerbation of renal dz - Hypersensitivities leading to bronchospasm may occur |
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Acetaminophen
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non-specific COX inhibitor not an NSAID
Analgesic and Antipyretic Extensively metabolized in the liver -> severe hepatotoxicity No stomach irritation!! :) |
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Ibuprofen (Advil)
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Non-selective Cox inhibitors
Anti inflammatory Analgesic Antipyretic More potent and expensive than aspirin but have milder GI effects CYP 2C9 Side effects: Regular use may decrease cardioprotective effect of aspirin |
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Naproxen (Aleve)
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Non-selective Cox inhibitors
Anti inflammatory Analgesic Antipyretic |
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Indomethacin
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Non-selective Cox inhibitors
Generally only used in gout, ankylosing spondylitis, pericarditis and pleurisy SE: Very severe gastric effects, HA, thrombocytopenia, aplastic anemia, coronary artery constriction, hyperK |
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Meclofenamate
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Non-selective Cox inhibitors
Similar to aspirin Less GI effects |
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Diclofenate
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Non-selective Cox inhibitors
Ointment for osteoarthritis and patch for minor injury Very high SE with oral use |
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Sulindac
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Non-selective Cox inhibitors
Prodrug |
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Phenylbutazone
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Non-selective Cox inhibitors
Not frequently used |
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Celecoxib (Celebrex)
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Selective, reversible inhibitor of COX2
CYP 2C9 inhibitor Much lower GI SE |
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Misoprostol
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synthetic prostaglandin
- can prevent gastric ulcers when used with a non-selective NSAID (DOC) SE: Cannot be used in pregnancy (causes termination) Severe diarrhea |
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Methotrexate
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Effects on lymphocytes (decrease proliferation, cytokine production)
Effects on PMNs (Decreased chemotaxis, free radical production) Inhibition of DHFR and thymidine deficiency - Low doses used in RA SE: GI, Hepatic and hematological effects Teratogenic |
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Hydroxychloroquine
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Partitions into the acidic vacuole
- Tx of malaria and ameba infestation - mild cases of RA - Reduces chemotaxis, phagocytosis and superoxide production in PMNs. - takes 3-6 mo for RA effects SE: No myelosuppressive effects - monitor vision for retinal changes - not for use with g6P DH deficiency SAFE to use during pregnancy. |
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Sulfasalazine
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sulfonamide
Split into 5-aminosalicylic acid and sulfapyridine in GIT MOA unknown - Tx of IBD - sulfapyridine absorbed -> anti RA effect SE: Rashes, dizziness, GI upset and photosensitivity are common Rare neutropenia |
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Leflunomide
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Active compound is dihydroorotate dehydrogenase
Insueing pyrimidine deficiency produces methotrexate-like action Hepatic metabolism to active compound CYP 2C9 inhibitor SE: Diarrhea Hair loss Hepatic damage |
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Azathioprine (Imuran)
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Converted to 6-mercaptopurine inhibitor of several steps in purine interconversions that inhibit DNA synth
Antirheumatic SE: May increase risk of lymphoma |
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Etanercept
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Fusion protein - human TNF rec and Fc fragment of IgG
Scavenges TNF TNF alpha inhibitor Reduce RA symptoms and joint damage Moderate to severe RA Dz from ankylosing spondylitis to psoriasis to UC Sub Q injection - Rapid onset of action - short half life - less potential for toxicity SE: opportunistic infections (TB) |
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Imifliximab
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Chimeric human-mouse monoclonal anti-TNF, reduces symptoms by inactivating TNF
Reduce RA symptoms and joint damage Moderate to severe RA Dz from ankylosing spondylitis to psoriasis to UC Used with methotrexate therapy increases effectiveness SE: opportunistic infections (TB) |
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Adalimumab
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human antibody
Reduce RA symptoms and joint damage Moderate to severe RA Dz from ankylosing spondylitis to psoriasis to UC Sub Q like imifliximab SE: opportunistic infections (TB) |
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Anakinra
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recombinant protein with point mutation
Competitive antagonist at IL-1R Marginally effective |
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Abatacept
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inhibits T cell activation by binding to CD80 and CD86 on APC to prevent binding of Tcell CD28
- RA tx Do not give with TNF inhibitors SE: opportunistic infections (TB) |
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Rituximab
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Targets B cell antigen CD20, antibody binding causes cell death by apoptosis
-used with methotrexate against autoimmune dz -IV infusion SE: infusion reactions, hep B activation and viral infections |
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Golimumab
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Human monoclonal antibody with high affinity TNF alpha
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Tocilizumab
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Humanized monoclonal antibody against IL-6 receptors
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Certolizumab
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Humanized, pegylated, Fc-free, monoclonal anti-TNF alpha
- approved for use in Crohns dz |
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Colchicine
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Binds tubulin in leukocytes and reduced their mobility and phagocytosis susceptibility
Use for short periods of time ONLY -TX: GOUT NSAID PO SE: - GI disturbances (D) - Hair loss - marrow depression - Peripheral neuropathy - myopathy... etc. |
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Allopurinol
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Inhibits xanthine oxidase
Inhibits both steps in production of urate Inhibits purines Given chronically to prevent Gout attacks May precipitate gout attack at first SE: - allergic skin reactions - GI disturbances - marrow depression - peripheral neuritis |
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Febuxostat
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Non-competitive inhibitor of xanthine oxidase which reduces urate
Reduces Urate levels in Gout pts used when allergy to allopurinol |
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Probenicid
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Inhibits both excretion and reaccumulation of urate in proximal tubule
Can be given chronically to prevent gout attacks Also inhibits the tubular secretion of some other drugs (penicillins, indomethicin and other NSAIDs) SE: Rare allergic dermatitis and aplastic anemia |
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Pegloticase
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Recombinant form of uricase, catalyses formation of allantoin from uric acid which reduces the purine load
Used in otherwise uncontrolled gout Most pts develop antibodies which reduce effectiveness and can cause anaphylaxis |
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Cortisol
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steroids - Bind to cytoplasmic rec in complex with HSP 90 which then enters nucleus and binds to DNA sequences called GREs. GRE leads to changes in mRNA transcription.
3 main effects: - metabolic - anti-inflammatory - sodium retentive (aldosterone-like) - Short term doses for anything from bites to asthma - Long term only for dz like lupus Natural |
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Dexamethasone
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steroids - Bind to cytoplasmic rec in complex with HSP 90 which then enters nucleus and binds to DNA sequences called GREs. GRE leads to changes in mRNA transcription.
3 main effects: - metabolic - anti-inflammatory - sodium retentive (aldosterone-like) - Short term doses for anything from bites to asthma - Long term only for dz like lupus Very potent anti-inflammatory, less sodium retention |
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Prednisone & Prenisolone
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steroids - Bind to cytoplasmic rec in complex with HSP 90 which then enters nucleus and binds to DNA sequences called GREs. GRE leads to changes in mRNA transcription.
3 main effects: - metabolic - anti-inflammatory - sodium retentive (aldosterone-like) - Short term doses for anything from bites to asthma - Long term only for dz like lupus Po, IV, topical At low levels bind to CBG, higher levels bind to albumin or exist as free drugs |
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Epinephrine
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Nonselective B2 Agonists
B2, B1 and alpha used to manage severe acute asthma attack effects on pulmonary function are rapid 5-15 min Sub Q and aerosol SE: undesirable cardiac stimulation |
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Ephedrine
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high B1 receptor affinity
Oral SE: tremor and undesirable cardiac stimulation |
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Isoproterenol
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B1 and B2
aerosol - instantaneous response SE: B1 causes undesirable cardiac stimulation |
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Albuterol
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Selective B2 agonists
Produce bronchodilation with few cardiac side effects Longer duration than non-selective drugs short acting |
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Levalbuterol
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Selective B2 agonists
Produce bronchodilation with few cardiac side effects Longer duration than non-selective drugs short acting |
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Pirbuterol
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Selective B2 agonists
Produce bronchodilation with few cardiac side effects Longer duration than non-selective drugs short acting |
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Formoterol
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Selective B2 agonists
Produce bronchodilation with few cardiac side effects Longer duration than non-selective drugs long acting |
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Salmeterol
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Selective B2 agonists
Produce bronchodilation with few cardiac side effects Longer duration than non-selective drugs Long acting |
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Formoterol fumarate
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Long acting beta 2 adrenergic receptor agonist
must be used with inhaled steroid COMBO inhalers |
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Levalbuterol
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R isomer of racemic albuterol
useful in pts refractory to racemic albuterol |
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Ipratropium Bromide
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anticholinergic agent
short-acting bronchodilator for chronic bronchitis and COPD Atrovent |
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Tiotropium Bromide
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inhalation powder
long-acting anticholinergic agent tx of bronchospasm associated with COPD--LONG acting (daily maintenance) |
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Theophylline
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increase CAMP
tx of prolonged asthma attack and COPD anti inflammatory effects PO for stages 1 and 2 asthma IV for stages 3 and 4 asthma SE: N/V. Contraindications: Do NOT use with barbituates or caffeine |
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Beclomethasone, Triamcinolone, budesonide, fluticasone propionate, mometasone furoate,flunisolide, ciclesonide
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Inhaled corticosteroids
- relieve or prevent airflow obstruction by anti-inflammatory action - not effective in relief of acute asthma attack |
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fluticasone propionate, budesonide
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Inhaled corticosteroids
- relieve or prevent airflow obstruction by anti-inflammatory action - not effective in relief of acute asthma attack Long duration of action, high local potency Used in combo inhalers with Long acting ones (Salmeterol and Formoterol) |
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Advair
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Combo inhalers with corticosteroid and long-acting beta 2 adrenergic agonist
improves lung function, decreases symptoms and exacerbations and reduces use of rescue short-acting beta 2 agonists Not for acute attacks |
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Symbicort
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Combo inhalers with corticosteroid and long-acting beta 2 adrenergic agonist
improves lung function, decreases symptoms and exacerbations and reduces use of rescue short-acting beta 2 agonists Not for acute attacks |
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Dulera
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Combo inhalers with corticosteroid and long-acting beta 2 adrenergic agonist
improves lung function, decreases symptoms and exacerbations and reduces use of rescue short-acting beta 2 agonists Not for acute attacks |
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Prednisone
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Mech poorly understood
- dramatic relief in severe asthma (stages III and IV) Oral or IV SE: suppression of hypothalamic-pituitary-adrenal function Cushing syndrome |
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Cromolyn sodium
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stabilizes mast cell membranes therefore inhibiting release of mediators
- prophylactic treatment of mild to moderate asthma Only effective when inhaled d/t poor GI absorption SE: - Very few - sore throat, dry mouth, skin rashes, HA, dizziness |
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Prostaglandins
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PGE1 and 2
- relax airway SM experimental |
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Zileuton
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Leukotriene synthesis inhibitor
asthma tx Not really used due to FDI |
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Montelukast
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Oral cysteinyl leukotriene D4 receptor antagonist
approved for allergic rhinitis |
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Omalizumab
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humanized monoclonal antibody given subQ that binds to IgE
use with moderate to severe asthma |
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Cromolyn sodium
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Blocks influx of divalent ions and release of histamine.
tx of asthma |
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Nedocramil
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Blocks influx of divalent ions and release of histamine.
tx of asthma |
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Compound 48/80
Polymyxin B |
act as ionophores and cause influx of calcium and histamine release
cause histamine release |
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Diphenhydramine HCl
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First Generation Histamine1 receptor blocker
Diphenhydramine HCl - anti-motion sickness Reduce symptoms of allergy, allergic rhinitis and urticaria Blocks synaptic relay in 8th cranial nerve for N/V associated with motion SE: sedation |
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Chlorpheniramine
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First Generation Histamine1 receptor blocker
Reduce symptoms of allergy, allergic rhinitis and urticaria SE: sedation |
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Dimenhydrinate
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First Generation Histamine1 receptor blocker
Reduce symptoms of allergy, allergic rhinitis and urticaria SE: sedation |
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Hydroxyzine HCl
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First Generation Histamine1 receptor blocker
Reduce symptoms of allergy, allergic rhinitis and urticaria SE: sedation |
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Meclizine HCl
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First Generation Histamine1 receptor blocker
Reduce symptoms of allergy, allergic rhinitis and urticaria SE: sedation |
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Promethazine HCl
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First Generation Histamine1 receptor blocker
Reduce symptoms of allergy, allergic rhinitis and urticaria SE: sedation |
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Astemizole
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Second generation H1 receptor blocker
BANNED IN THE US |
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Fexofenadine
Loratidine Desloratadine Cetirizine Levocabastine Acrivastine |
Second Generation Histamine1 receptor blockers
Reduce symptoms of allergy, allergic rhinitis and urticaria Without the drowsy side effect of first generations |
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Sodium bicarbonate
Calcium carbonate |
Gastric/peptic ulcers
Esophageal reflux Hypersecretion of HCl Antacids - weak bases that inactivate HCl and might also confer some mucosal protection via stimulaltion of mucosal prostaglandin production |
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Magnesium hydroxide
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Gastric/peptic ulcers
Esophageal reflux Hypersecretion of HCl Antacids - weak bases that inactivate HCl and might also confer some mucosal protection via stimulaltion of mucosal prostaglandin production SE: Diarrhea |
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Aluminum hydroxide
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Gastric/peptic ulcers
Esophageal reflux Hypersecretion of HC lAntacids - weak bases that inactivate HCl and might also confer some mucosal protection via stimulaltion of mucosal prostaglandin production SE: constipation |
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Magnesium trisilicate
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Gastric/peptic ulcers
Esophageal reflux Hypersecretion of HCl Antacids - weak bases that inactivate HCl and might also confer some mucosal protection via stimulaltion of mucosal prostaglandin production |
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Cimetidine/Tagamet
Ranitidine/Zantac Famotidine/Pepcid Nizatidine |
H2 receptor blockers
Diminish gastric secretion Tx of duodenal and gastric ulcers - gastritis - reflux esophagitis |
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esomeprazole (Nexium)
lansoprazole (Prevacid) pantoprazole (Protonix) omeprazole (prilosec) |
activated in acidic environment so don’t use antacid with this!
Gastric and duodenal ulcers Interaction with plavix!!! Proton pump inhibitors - irreversibly inhibits gastric parietal cell proton pump |
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Octreotide
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Somatostatin analog - inhibits gastric acid secretion
Gastric and duodenal ulcers IV administration required |
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Sucralfate
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Barrier agent - inhibits pepsin and bile action without changing pH. Coats the ulcer bed. MOA?
Gastric and duodenal ulcers |
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Bismuth subsalicylate
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binds to ulcer, coats and protects from acid and pepsin
GI ulcers H. pylori especially Pepto-bismol - especially useful with abx for H. pylori |
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Misoprostol
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DOC for ulcers from NSAIDs
DO NOT used in pregnancy--will cause uterine contraction/pregnancy termination |
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Metoclopramide
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cholinomimetic activity which stimulates motility of UGI while increasing tone of LES
TX: GI Motility anti-emetic reflux esophagitis Reglan SE: Tardive dyskinesia |
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Amoxicillin
Clarithromycin Bismuth subsalicylate Tetracyclin Metronidazole |
Tx of H. pylori usually involves:
1. two antibiotics 2. a proton pump inhibitor Abx for H. pylori Cheap but tedious regimen: 1. Bismuth 2. metronidazole 3. H2 blocker 4. tetracycline |
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Ipecac
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emetic agent
not used much anymore d/t harmful nature of regurgitation of toxins |
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Apomorphine
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Central acting emetic
emetic agent usually use gastric lavage instead |
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Ondansetron
Granisetron |
5-HT3 antagonists
Anti-emetic Zofran Granisol |
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Aprepitant
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Neurokinin receptor antagonist
Anti-emetic Emend |
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Prochlorperazine
Trimethobenzmide Metochlopramide |
“others”
Anti-emetic Compazine Tigan Reglan |
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Castor oil
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Hydrolyzed to ricinoleic acid by lipases from pancreas - acid stimulates GI motility and promotes evacuation
Laxative Contraindication: Do not use in pregnancy as it may induce premature labor |
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Emodin alkaloids
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Metabolized by GI bacteria to active compound that stimulates peristalsis
Laxative Cascara, senna, aloes |
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Diphenylmethanes
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potent irritants and stimulatory agents
Laxative Phenolax, Exlax |
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magnesium sulfate
magnesium hydroxide |
Osmotic laxatives
Laxatives Epsom salts Milk of Mag - also used as antacid |
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psyllium seed
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Fiber laxative
Laxative Metamucil, Konsyl |
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Diphenoxylate
atropine loperamide |
Motility agents
Lomotril Immodium |
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Kaolin
pectin Bismuth salicylate |
Absorbent powders - absorb water, toxins and provide protective coating to GIT
tx of GI distress |
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Donnagel
Kaopectate |
Combo products
GI distress Kaolin magma and belladonna Kaolin magma and pectin |
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Prednisone & Prednisolone
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- Inhibit production of IL-1,2 &4 and TNF to reduce cytokine-induced inflammation
- Inhibit TLC proliferation and induce lymphocyte and eos apoptosis - Inhibit monocyte and mac activation, chemotaxis and recognition of antigen - Inhibit neutrophil chemotaxis and adhesion to endothelium - Inhibit Phospholipase A2 and COX2 to suppress proinflammatory prostaglandins, leukotrienes, thromboxanes and Platelet Activating Factor Uses: - autoimmune dz like: RA, asthma, IBD, allergies, inflammatory skin dz - solid organ transplant - stem cell transplant - GVHD SE: Skin and soft tissue - cushings syndrome Ocular - cataracts Vascular - atherosclerosis and hypertension GI - gastritis and PUD MS - osteoporosis Neuro - psychosis at high doses Infections Endocrine - DM, Growth delay, HLD, wt gain GU: amenorrhea/anovulation/infertility |
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Cyclosporine
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Calcinurin inhibiting agent
lipophilic cyclic decapeptide - binds cyclophilins Uses: Immunosuppression d/t binding of calcineurin, which inhibits dephosphorylation of nuclear factors in cytoplasm and inability to translocate to nucleus = reduced transcription of early cytokine gene IL-2, 3, 4, TNF alpha and gamma and GM-CSF CYP 3A4 elimination (SEE LIST on p. 209) PO, IV, Topical and opthalmic Both cross placenta and Breast milk SE: Nephrotoxicity at therapeutic and low levels |
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Tacrolimus
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Calcinurin inhibiting agent
non-antibiotic macrolide - binds FKBPs Immunosuppression d/t binding of calcineurin, which inhibits dephosphorylation of nuclear factors in cytoplasm and inability to translocate to nucleus = reduced transcription of early cytokine gene IL-2, 3, 4, TNF alpha and gamma and GM-CSF CYP 3A4 elimination (SEE LIST on p. 209) PO, IV, Topical and opthalmic Tacrolimus is preferred in liver transplant d/t cyclo’s need for bile salts Both cross placenta and Breast milk SE: Nephrotoxicity!!! |
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Sirolimus
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macrolide non-antibiotic produced by a fungus that binds immunophilins and interferes with signal transduction pathways elicited by IL2, binds FKBP and inhibits mTOR -> Tcells arrest in G1
Uses: Immunosuppression CYP 3A4 elimination (list on 209) usually used in combo with cyclosporine SE: impaired wound healing lymphoceles HLD thrombocytopenia synergistic nephrotox |
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Azathioprine
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cytotoxic agent, anti-metabolite
Converted to 6-MP by glutathione which in metabolized in cells and changes RNA synthesis -> decrease in B and T lymphocyte numbers, immunoglobulin production and IL-2 secretion Uses: Immunosuppression - autoimmune disorders - organ transplant SE: Potentially lethal DDI with allopurinol - bone marrow suppression - anemia - alopecia - GI distress |
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Methotrexate
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Structural analog of folic acid, completely binds DHFR and decrease the amount of FH4 which effects purine and pyrimidine metabolism
Uses: RA and psoriasis GVHD PO, IV, and IM Increased toxicity with other folate depleting drugs like TMP/SMX or probenecid SE: - GI upset - alopecia - macrocytosis - CNS - fatigue, HA and loss of concentration - Toxicity can be fatal! |
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Mycophenolate Mofetil
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Inhibits antibody formation
Renal or other solid organ transplants SE: GI distress |
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Leflunomide
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inhibitor of pyrimidine synthesis
Uses:RA PO SE: diarrhea liver damage kidney impairment teratogenic |
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Cyclophosphamide
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alkylating agent
metabolized in liver to produce aldophosphoramide -> interfere with nucleic acid chains Uses: severe, life-threatening autoimmune dz (lupus, RA, vasculitis etc) - DDI with drugs that alter hepatic microsomal enz - DDI TCAs - DDI with succinylcholine SE: -N/V - Alopacia - anorexia - D - stomatitis and mucositis |
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ATG
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Abs raised to human lymphoid cells
“Anti-thymocyte globulin” Uses: induce immunosuppression Organ transplant SE: - infection - fever - HA - lymphoma |
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ATGAM
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lymphocyte immune globulin
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Muromonab- CD3
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Anti CD3 antibody
Inactivate, deplete and destroy T cells Uses: organ transplants SE: cytokine release d/t antibody activation and destruction of T cells |
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Rho
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Immune globulin
Rhogam |
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Adalimumab
Infliximab Etanercept |
Anti TNF alpha agents
Uses: Autoimmune dz, RA, psoriasis and Crohns recombinant monoclonal ab chimeric monoclonal ab antibody-TNF alpha receptor fusion protein |
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Daclizumab
Basiliximab |
Anti-cytokine antibodies bind CD25 IL-2 receptor
Prevention of organ rejection via immunosuppression |
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Hemicholinum 3
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Blocks transport of choline into nerve terminal
no therapeutic use |
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Botulinum toxin
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Prevents Ach release from nerve terminal
Also, tx of BPH and drooling in Cerebral palsy |
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Acetylcholine
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QUAT-Cholinergic Agonist -
muscarinic and nicotinic receptors vasodilation |
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Atropine
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Muscarinic antagonist
natural alkaloid causes tachycardia tx of travellers diarrhea, bladder retention, and dries secretions |
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scopolamine
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Muscarinic antagonist
anti-motion sickness tx sedation can use as a patch |
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benztropine
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muscarinic antagonist
tx PD tremor and rigidity PO less SE sedation |
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pilocarpine
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TERT - Muscarinic agonist
Ophthalmic Causes Miosis, tx for chronic glaucoma, Stimulates secretions |
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carbachol
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QUAT - muscarinic and nicotinic agonist
Causes Miosis (during lens replacement surgery) topical only due to wide spread effects CARBon copy of Ach |
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tropicamide
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Muscarinic Antagonist
causes mydriasis Used during an eye exam for dilation |
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Bethanechol
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QUAT - musc Agonist
mostly muscarinic activity with long duration of action Mostly acts on GIT and bladder (on detrussor to stim) Tx of stasis of GIT, urinary bladder, esp. post-partum and after general anesthesia |
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Propantheline
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QUAT - musc antagonist
spasmolytic in GIT, biliary tract and bladder (decreases GI motility) |
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Oxybutynin
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TERT - musc antagonist
relief of bladder spasm Tx urinary urgency available in transdermal patch CYP 3A4 |
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neostigmine
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QUAT- mAchR agonist
indirect acting inhibitor of AchE Tx for myasthenia gravis and for stimulating GI motility (similar to Bethanechol) |
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Tolterodine
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TERT - mAchR antagonist (in bladder)
Tx of urinary frequency CYP 2D6 |
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Trospium
Solifenacin Darifenacin |
Muscarinic Antagonists
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Methacholine
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QUAT - muscarinic agonist
Dx of bronchial airway hyper-reactivity Bronchial constriction suppression of atrial tachycardia tx of acute respiratory distress ONLY USE WITH PROPER MEDICAL TX AVAILABLE D/T RESP DISTRESS!!! |
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Ipratropium
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Quat - Muscarinic Antagonists
Tx of COPD (emphysema and chronic bronchitis) Atrovent |
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Tiotropium
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Quat - Muscarinic Antagonists
Tx of COPD (emphysema and chronic bronchitis) Spiriva - longer t1/2 |
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Nicotine
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TERT natural alkaloid/insecticide. Lipid soluble.
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Varenicline
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Nicotinic receptor partial agonist
smoking cessation Chantix |
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d-tubocurarine
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Competitive antagonist
NICOTINIC BLOCKING AGENTS prototype drug, natural alkaloid Effects reversed by neostigmine & erdophonium. decreases BP, decreases TPR via histamine. |
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Cistracurium
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Competitive Antagonist
NICOTINIC BLOCKING AGENT synthetic, spontaneous breakdown in plasma, short half life (20 minutes) Laudanosine, a breakdown product, may excite CNS and cause seizures |
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Pancuronium
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steroid based competitive nAchR antagonist
NICOTINIC BLOCKING AGENT Long duration of action renally eliminated SE: tachycardia |
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Vecuronium
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steroid based competitive antagonist with good nmj selectivity
NICOTINIC BLOCKING AGENT little effect on cardiovascular system intermediate duration of action (30 minutes) hepatic elimination |
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Rocuronium
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Fastest onset competitive non-depolarizing antagonist
NICOTINIC BLOCKING AGENT for rapid sequence intubation can prevent fasiculations when given before/with SuCh biliary excretion minimal CV effects |
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Succinylcholine
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Agonist - Depolarizing Blocking Agent acting primarily at NMJ
NICOTINIC BLOCKING AGENT Liberates histamine Used for intubation - promotes skeletal muscle relaxation (usually lasts 5 minutes in single dose) Plasma pseudocholinesterase metabolized very rapid onset of action Single dose = phase 1 blockade Continuous = phase 2 blockade (reversed by neostigmine and erdophonium) SE: localized muscle fasiculations (give rocuronium before this to help) |
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Edrophonium
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QUAT-Anti AchE.
Use to diagnose myasthenia gravis. Can reverse a phase II blockade |
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Dantrolene
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Blocks release of Ca from SR
spasmolytic Uses: - spasticity in pts already confined to wheelchair - malignant hyperthermia during anesthesia causes significant muscle weakness |
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Baclofen
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Agonist at GABA B receptors, activation leads to hyperpolarization, decreases presynaptic excitatory neurotransmission
Anti spasmodic |
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Tizanidine
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atypical agonist at alpha 2 rec
probably increases both pre and post synaptic inhibition Spasmolytic |
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Riluzole
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Inhibitor of glutaminergic signaling
Prolongs life in ALS pts |
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Cyclobenzaprine
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MOA unknown
tx of acute muscle spasms after trauma SE: significant anti muscarinic and sedative activities |
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hexamethonium
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Ganglionic blocking agent
was one of the first drugs used to treat hypertension |
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Mecamylamine
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Secondary amine
Ganglionic blocker |
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Physostigmine
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Reversible Anticholinesterase Agents
Either bind non-covalently to active site of AchE or are slowly hydrolyzed by the enzyme = temporary inhibition TERT- use topically for glaucoma (miosis), metabolized in the plasma |
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Neostigmine
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Reversible Anticholinesterase Agents
Either bind non-covalently to active site of AchE or are slowly hydrolyzed by the enzyme = temporary inhibition QUAT- direct mAchR Increases GI motility and stimulates the detrussor muscle. Also a tx for myasthenia gravis |
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Pyridostigmine
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Reversible Anticholinesterase Agents
Either bind non-covalently to active site of AchE or are slowly hydrolyzed by the enzyme = temporary inhibition QUAT-Longer duration, oral DOC for myasthenia gravis Prophylactic tx for nerve gas (sarin) |
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Edrophonium
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Reversible Anticholinesterase Agents
Either bind non-covalently to active site of AchE or are slowly hydrolyzed by the enzyme = temporary inhibition QUAT--single bolus lasts 5 minutes, used in diagnosis of myasthenia gravis Can reverse nicotinic receptor block, Phase II (caused by curare) |
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Rivastigmine
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Reversible Anticholinesterase Agents
Either bind non-covalently to active site of AchE or are slowly hydrolyzed by the enzyme = temporary inhibition TERT-Alz treatment Few DDI's |
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Donepezil
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Reversible Anticholinesterase Agents
Either bind non-covalently to active site of AchE or are slowly hydrolyzed by the enzyme = temporary inhibition TERT-Alz tx, longer duration, P450 metabolism, mild SE's |
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Galantamine
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Reversible Anticholinesterase Agents
Either bind non-covalently to active site of AchE or are slowly hydrolyzed by the enzyme = temporary inhibition TERT-natural, Alz tx |
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Tacrine
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Reversible Anticholinesterase Agents
TERT-1st Alz drug-no longer used due to hepatotoxicity |
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Echothiophate
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Irreversible cholinesterase inhibitor
Organophosphate Miosis with ophthalmic use, topically (lasting 3 days) Causes lens clouding |
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Malathion
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Irreversible cholinesterase inhibitor
Insecticide Used against lice liver metabolism |
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Parathion
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Irreversible cholinesterase inhibitor
Insecticide Used in farming only, absorbed through the skin causes increased GI motility, increased secretions, hypotension, bradycardia, bronchospasms and convulsions. |
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Sarin
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Irreversible cholinesterase inhibitor
nerve gas causes increased GI motility, increased secretions, hypotension, bradycardia, bronchospasms and convulsions. Treat prophylactically with pyridostigmine. Treat post exposure with atropine and pralidoxime. |
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Pralidoxime
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AChE Regenerator
QUAT-splits off the organophosphate. Treatment for post nerve gas/organophosphate exposure. |
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Vinblastine
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Vinca alkaloid that can block NE transport in the nerve axon
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Isoproterenol
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synthetic catecholamine
Uses beta receptors only. |
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Alpha Agonists
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ALPHA 2: Clonidine > alpha-methyl-NE >> oxymetazoline
ALPHA 2 = 1: Naphazoline = NE = EPI ALPHA 1: Phenylephrine (PE) > methoxamine |
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Clonidine
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Alpha 2 agonist
lowers BP, reduces sympathetic outflow to blood vessels. Treatment for essential hypertension. Need to taper to D/C Other forms reduce intraocular pressure SE: dizziness, nausea, impotence, dry mouth |
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Alpha-methyl-NE
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Alpha agonist (mainly alpha 2).
Synthesized from methydopa. Enters CNS readily. Has much lower affinity for Beta receptors than NE. Reduces renal vascular resistance. |
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Fenoldopam
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Dopamine D1 agonist
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Bromocriptine
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D2 agonist and Partial D1 agonist
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Phenylephrine
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Alpha receptor agonist only.
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Pergolide
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D1 and D2 agonist
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Pramipexole
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D2 agonist
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Ropinirole
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D2 agonist
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Tyramine
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Indirectly acting sympathomimetic drug
Do not use with MAO’s. |
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Amphetamine
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Indirectly acting sympathomimetic drug
Can induce tolerance/tachphylaxis. |
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ephedrine
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Indirectly acting sympathomimetic drug
Can induce tolerance/tachphylaxis. |
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Alpha methyl tyrosine
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TH inhibitor which inhibits the formation of DOPA
NOT USED IN USA |
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Reserpine
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Produces progessive tissue loss of NE which impairs adrenergic function in ANS and CNS
Blocks VMAT Uses: Management of essential HTN NOT really used anymore SE: miosis salivation GI hypersecretion peptic ulceration hyperperistalsis, diarrhea bradycardia hypotension emotional depression and tremors |
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Clonidine
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Agonist of alpha 2 receptors
lowers BP |
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Guanthidine
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taken up by SS neurons, reduces NE storage, blocks AP transmission, blocks NET
Uses: Lowers BP, HR and renin secretion SE: marked postural hypotension |
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Methyldopa
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metabolized in CNS, much higher affinity for alpha2 than alpha1
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TCAs
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Block NET, weak inhibitor of 5-HT transporter
Thus enhance actions of NE and 5-HT Uses: Antidepressants SE: - tremor - insomnia - blurred visio - orthostatic HoTN |
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Cocaine
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reversibly binds NET and reuptake of DA marked enhancement of response to NE, EPI and DA
Uses: stimulation of CNS, block nerve conduction (local anesthesia in high concentrations) |
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Dobutamine
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adrenergic agonist
racemic - alpha 1 cancels out left with only beta 1 agonist Uses: acute management of heart failure to improve CO |
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Phenoxybenzamine
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noncompetitive irreversible alpha adrenergic antagonist
Uses: - pheochromocytoma - HTN - Raynauds syndrome |
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Phentolamine
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competitive reversible antagonist
Uses: HTN control in pts with pheochromocytoma Tx of HTN crisis following abrupt removal of clonidine or tyramine FDI |
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Prazosin
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selective antagonist of alpha 1
Uses: lowers BP, tx of primary HTN CHF - decreases preload and afterload |
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Yohimbine
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Alpha 2 blocker
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Doxazosin
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increased t/12 over prazosin
blocks alpha 1 receptors |
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Propranolol
Carteolol Levobunolol Nadolol Pindolol Timolol Penbutolol |
Beta Blockers
Selective competitive beta-receptor antagonist Blockade of B1 receptors -> decrease in HR and CO and sinus rate, slows conduction Blocks exercise induced changes in cardiac parameters Beta 2 blockade may initially increase peripheral resistance Block release of renin from JG apparatus-> anti-HTN Reduce peripheral effects of hyperthyroidism d/t block of SS activity Reduce intraocular pressue in glaucoma manage anxiety Prophylaxis of migraine HA SE: Can worsen asthma Can worsen CHF, Raynauds and DM Never use with Ca blockers -> AV block Withdraw gradually |
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Acebutolol
Atenolol Betaxolol Esmolol Metoprolol |
Cardiac Selective Beta blockers
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Labetelol
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Blocks both alpha and beta receptors with greater affinity for Betas (3:1)
Lowers peripheral vascular resistance without a major change in the heart rate or cardiac output. Has some intrinsic activity (partial agonist) and good membrane stabilizing action (local anesthetic like action). |
