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    Musculoskeletal Drugs

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    janul
    1. Glucocorticoids and NSAIDs are used to treat inflammation by inhibiting prostaglandin production through different mechanisms of action. Their use can cause side effects affecting the GI tract, liver, kidneys, cardiovascular and metabolic systems. 2. Muscle relaxants are classified based on their sites and mechanisms of action. Commonly prescribed types include antispastic agents like baclofen and antispasmodics like carisoprodol which have central nervous system effects. They are associated with side effects like drowsiness. 3. Injections of steroids can treat musculoskeletal disorders but have risks of complications with prolonged use and should be done carefully in certain groups like the elderly. NSA

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    Musculoskeletal Drugs

    Uploaded by

    janul
    146 views29 pages
    1. Glucocorticoids and NSAIDs are used to treat inflammation by inhibiting prostaglandin production through different mechanisms of action. Their use can cause side effects affecting the GI tract, liver, kidneys, cardiovascular and metabolic systems. 2. Muscle relaxants are classified based on their sites and mechanisms of action. Commonly prescribed types include antispastic agents like baclofen and antispasmodics like carisoprodol which have central nervous system effects. They are associated with side effects like drowsiness. 3. Injections of steroids can treat musculoskeletal disorders but have risks of complications with prolonged use and should be done carefully in certain groups like the elderly. NSA

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    1. Glucocorticoids and NSAIDs are used to treat inflammation by inhibiting prostaglandin production through different mechanisms of action. Their use can cause side effects affecting the GI tract, liver, kidneys, cardiovascular and metabolic systems. 2. Muscle relaxants are classified based on their sites and mechanisms of action. Commonly prescribed types include antispastic agents like baclofen and antispasmodics like carisoprodol which have central nervous system effects. They are associated with side effects like drowsiness. 3. Injections of steroids can treat musculoskeletal disorders but have risks of complications with prolonged use and should be done carefully in certain groups like the elderly. NSA

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    © All Rights Reserved
    Download as PPT, PDF, TXT or read online from Scribd
    Download as ppt, pdf, or txt
    146 views29 pages

    Musculoskeletal Drugs

    Uploaded by

    janul
    1. Glucocorticoids and NSAIDs are used to treat inflammation by inhibiting prostaglandin production through different mechanisms of action. Their use can cause side effects affecting the GI tract, liver, kidneys, cardiovascular and metabolic systems. 2. Muscle relaxants are classified based on their sites and mechanisms of action. Commonly prescribed types include antispastic agents like baclofen and antispasmodics like carisoprodol which have central nervous system effects. They are associated with side effects like drowsiness. 3. Injections of steroids can treat musculoskeletal disorders but have risks of complications with prolonged use and should be done carefully in certain groups like the elderly. NSA

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    © All Rights Reserved
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    Download as ppt, pdf, or txt
    of 29

    Learning objectives

    1.be able to describe action mechanisms and side


    effects of glucocorticoids and nonsteroiadal anti-
    inflammatory drugs and enumerate complications
    and contraindications of local glucocorticoid
    administration.
    2. be able to describe muscle relaxants
    classification according to their action mechanisms
    (define antispastic and spasmolytic drugs), and
    describe clinical usage and side effects.
    Non- Streoidal Anti-Inflammatory
    Drugs (NSAIIDs)
    Benefical effects:
    Analgesia
    Antipyresis (inhibits PGs in CNS)
    Antiinflammatory
    Antiplatelet (prevents thromboxane A2
    production)
    Mechanism
    Inhibiton of the cyclo-oxygenase (COX)
    Decrease in prostoglandin production
     Cox-1: stomach, intestine, platelet, kidney
     Cox-2: involved in inflammation
    Inhibition of lipoxygenase (sulindac,
    diclofenac)
    Inhibiton of neutrophil adhesion (aspirin,
    indomethacin)
    Inhibition of cytokine production
    Classification
    Salicylates Anthranilic acid
     Aspirin Mefenamic acid
     Diflunisal Sulfananilides
    Para-aminopheno Nimesulid
     Acetaminophen
    Heteroaryl acetic acid
    Diclofenac
    Acetic acids
    Ketolorac
     Indomethacin
    Arylpropionic acid
     Sulindac
    Ibuprofen
     Etodolac
    Naproxen
    Ketoprofen
    Classification
    Enolic acid Cox-2 selective
     Piroxicam Etodolac
     Meloxicam Diclofenac
    Alkanones Nabumetone
     Nabumetone
    Meloxicam
    Coxib
     Celecoxib
     Etoricoxib
     Lumiracoxib
    Side effects
    Hepatotoxicity Nephrotoxicity
     İdiosynchratic hepatit  Papillary necrosis

    (indomethacin,  İncreased sodium

    diclofenac) retantion
     Cholestasis  Decreasing GFR

    GİS  Acute tubular necrosis

     Dyspepsia  Acute intersititial

     GOR nephritis
     Peptic ulcer

     Hemorrhage
    Who is at risk for GD ulcers
    Elderly
    History of PU
    Higher dosage
    Chronic diseases
    Anticoagulant therapy
    Corticosteroid use
    Tobacco and alcohol
    Protection
    Misoprostol (PGE1 analog)
    Proton Pump inhibitors
    Glucocorticoids(GC)
    GC are widely used for the suppression of
    inflammation in chronic inflammatory
    diseases such as asthma, RA,
    inflammatory bowel disease and
    autoimmune diseases.
    GC inhibit the expression of multiple
    inflammatory genes
    Glucocorticoids(GC)
    GC increase the syntesis of lipocortin-1,
    that has inhibitory effect on phospholipas
    A2 and therefore inhibit the production of
    lipid mediators as well as inhbit genes
    coding for COX-2.
    Some commonly used
    glucocoticoids
    Equivalent oral dose(mg)
    Cortisol 20
    Prednisolone 5
    Methylprednisolone 4
    Triamcinolone 4
    Dexamethasone 0.75
    Dosing (EULAR)
    Low dose up to 7.5 mg/d
    Medium dose > 7.5 but ≤ 30 mg/d
    High dose >30 but ≤ 100 mg/d
    Advers Effects
    Bone and muscle:
    Osteoporosis
    Mean first- year loss of bone ranging from
    1.5-20% at the dose range ≤ 10 mg/d
    prednisolone.
    Addition to GC theraphy Ca and vit D or
    bisphosphonate should recieve to patient.
    Osteonecrosis
    Myopathy
    Advers Effects
    Cardiovascular:
    Fluid retention (Hypertension)
    Affect lipid profile
    Premature atherosclerotic vascular
    disease
    Cardiac arrythmias
    Advers Effects
    Dermatologic and appearance
    Skin thinning
    Ecchymoses
    Cushingoid appearance
    Hirsutism
    Stria
    Impair wound healing
    Weight gain
    Advers Effects
    Gastrointestinal Metabolic and
    Gastritis endocrine
    Ulcers DM
    Gastrointestinal HPA insufficiency
    bleeding Neuropsychiatric
    Infectious diseases Imsomnia
    Ophtalmologic Memory impairment
    Cataracts Depression
    Increased intra-ocular Psychosis
    pressure
    Injections of steroids

    These more invasive therapeutic methods


    are recognized for the treatment of many
    disorders of the musculoskeletal system.
    However, except in certain rare cases,
    their use over a prolonged period is not
    recommended.
    Complications The physician should
    Hemarthrosis, also recommend that
    Exacerbation of the the patient not put
    inflammation and pain, any undue tension on
    Infection, tendons close to the
    Soft tissue atrophy injection site so
    Thinning of the skin as to prevent their
    Changes in skin possible rupture
    pigmentation.


    Contraindications
     Any localized or generalized infectious
    process,
     Fracture, the wearing of a joint brace,
     Coagulation problems,
     No relief after the first injection.
    Muscle relaxants

    The effectiveness of these medications is


    much debated.
    But it is particularly important to show
    prudence when the subjectis elderly, and
    to write prescriptions that take into
    account the following adverse side effects:
    drowsiness, confusion, anticholinergic
    effects
    Classification

    Peripherally acting (Neuromuscular


    blockers)
    Centrally acting
    Baclofen -Diazepam
    Direct acting
    Dantrolene
    Spasmolytic agents

    Spasticity-characteristics
    Increased tonic stretch reflexes
    Increased flexor muscle spasm
    Muscle weakness
    Clinical conditions of spasticity:
    Cerebral palsy, Multiple sclerosis, Stroke
    Clinical spasticity:
    Reflex arc involvement
    Higher center affects descending pathways leading to alpha
    motoneurons hyperexcitability
    Mechanisms (↓ spasticity)
    – Alteration in stretch reflex arc
    – Attenuation of excitation-contraction coupling
    SPASMOLYTIC DRUGS

    (Central effect)
    Diazepam
    Baclofen
    Tizanidine
    Dantrolene
    Carisoprodol (Soma, Rela)
    chlorphenesin (Maolate)
    chlorzoxazone (Paraflex)
    cyclobenzaprine (Flexeril)
    metaxalone (Skelaxin)
    methocarbamol (Robaxin)
    orphenadrine (Norflex)
    Skeletal
    There are 2 main categories of skeletal muscle
    relaxants: antispastic (such as baclofen or
    dantrolene) for conditions such as cerebral palsy
    and multiple sclerosis and antispasmodic agents
    for musculoskeletal conditions.
    The most commonly prescribed antispasmodic
    agents are carisoprodol, cyclobenzaprine,
    metaxalone, and methocarbamol.
    In comparison trials, no single skeletal muscle
    relaxant has been proven to be superior to
    another
    The most widely studied agent is
    cyclobenzaprine, with demonstrated efficacy for
    various musculoskeletal conditions but with
    significant sedation
    Tizanidine, which also causes marked sedation,
    or cyclobenzaprine may be useful in patients with
    insomnia because of severe muscle spasms.
    All skeletal muscle relaxants are
    associated with adverse effects including
    dizziness and drowsiness,

    Although methocarbamol and metaxalone


    are less sedating than tizanidine and
    cyclobenzaprine, evidence is limited for
    their efficacy.
    A specific skeletal muscle relaxant should
    be chosen according to consideration of
    adverse effect profile, patient preference,
    potential for abuse, and possible
    interactions with other prescribed
    medications because comparable efficacy
    data are limited.
    Despite their popularity, skeletal muscle
    relaxants should not be the primary drug class of
    choice for musculoskeletal conditions,"
    The American Pain Society and the American
    College of Physicians recommend using
    acetaminophen and...NSAIDs as first-line agents
    for acute low back pain and reserving skeletal
    muscle relaxants as an alternative treatment
    option.
    Skeletal muscle relaxants are better than
    placebo, but not more effective than NSAIDs in
    patients with acute back pain.

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