ATI musculoskeletal pharmacology

Rheumatoid Arthritis (RA)
Inflammatory disease of joints the joints, their surrounding structures, and other parts of the body. Typically develops in older adults but children can also have.

Rheumatoid Arthritis can result in
Joint stiffness, pain, swelling, deformities

Goals of drug therapy for rheumatoid arthritis are
Decrease pain and inflammation, and prevent deformities

Is the loss of calcium from bones, which make them porous and fragile

Common causes of osteoporosis
Menopause (less estrogen production), aging, long term glucocorticoid therapy (decreases the calcium the intestines absorb and increases the calcium the kidneys excrete), conditions that do not allow weight bearing (such as paralysis), poor calcium intake, chronic alcohol abuse, Paget’s disease (effects development of bone), decrease in bone density.

Goal of drug therapy for osteoporosis
Prevent excessive loss of calcium from bones, prevent fractures (most common sites of fractures are hip, wrist, spinal vertebra)

Myasthenia Gravis (MG)
A disease of the motor division of the peripheral nervous system. It is a autoimmune disease that destroys acetylcholine receptor sites on muscle fibers

Goal of treatment of Myasthenia Gravis
Increase the amount of acetylcholine at the neuromuscular junction for muscle contraction in order to decrease muscle weakness.

Types of drugs to treat rheumatoid arthritis
Nonsteroidal anti-inflammatory drugs (NSAIDs), glucocorticoids, disease-modifying antirheumatic drugs (DMARDs).

Disease-modifying Antirheumatic drugs (DMARDs) decrease
Joint inflammation, joint damage. Initially give along with NSAIDs because of slow onset of therapeutic effect of the DMARDs. Can discontinue the NSAIDs once the DMARDs start working

Autoimmune diseases
Disease in which the patients own antibodies attacks the patients own tissue

Disease-modifying antirheumatic drugs (DMARDs I)
Are anti-metabolite drugs which exert their therapeutic effect by interfering with the normal metabolic process.

Disease-modifying antirheumatic drugs (DMARDs I) in Rheumatoid arthritis
DMARDs I drugs interfere with production of lympthocytes or antibodies which stimulate the immune response

DMARDs I expected pharmacologic action
Immunosuppression, can slow or stop the progression of RA, also treats cancers but in much larger doses

disease-modifying antirheumatic drugs DMARDs I
Major nonbiologic. It’s antimetabolite drug that interferes with a normal metabolic process

Protype for DMARDs I drugs.

leflunomide (Arava)
DMARDs I drug

DMARD I side and adverse effects
Hepatotoxic causing liver damage, cause bone marrow suppression which results in a decrease in platelets, red and white blood cells, increased risk of infection, gastrointestinal ulceration, pulmonary fibrosis.

Methotrexate pregnancy catagory

Leflunomide (Arava) pregnancy catagory

DMARDs I interventions
Monitor patients for decreased playlets, decreased white and red blood cells, monitor for infection, monitor for liver problems and jaundice due to the hepatotoxicity of these drugs, if taking methotrexate assess for gastrointestinal bleeding

DMARDs I Administration
Only administer methotrexate once a week with patients with RA. Can prescribe folic acid supplement to help decrease the risk of toxicity

DMARDs I Patient instructions
Drink 8 to 12 8oz glasses of water daily, report yelling of skin or eyes, signs of infection, ulcerations of mouth or tongue, abnormal bleeding, bruising, or petechiae which are pinpoint spots of blood under the skin, blood in stool or vomitus, difficulty breathing or shortness of breath. Avoid pregnancy and ingestion of alcohol

DMARDs I precautions
Take caution when giving to patients with active bacterial or viral infections, people with peptic ulcer disease or with ulcerative colitis so monitor for pain and gastrointestinal bleeding

DMARDs I contraindications
Since these drugs can cause liver and kidney damage they are contraindicated for patients with liver insufficiency, hepatitis, renal insufficiency and WOMEN WHO ATE PREGNANT SHOULD NEVER TAKE THESE DRUGS BECAUSE OF DAMAGE TO FETUS. Do not breastfeed while taking either.

Taking Methotrexate and digoxin at the same time can
Reduce digoxin levels

Use of methotrexate with NSAIDs, salicylates, and sulfonamides may cause

Taking DMARDS I drugs and drinking alcohol can
Increase risk of hepatotoxicity

Disease-modifying antirheumatic drugs (DMARDs II )
Aka major biologic DMARDs.

Etanercept (Enbrel)
Prototype for DMARDs II drugs

Are cells that form new bone or bone remodeling

Cells that cause none reabsorption or bone loss

Infliximab (Remicabe)
DMARDs II drug

Adalimumab (Humira)
DMARDs II drug

Expected pharmacologic action of DMARDs II drugs
immunosuppression, these drugs suppress inflammation but in a different way then DMARDs I drugs, these drugs are tumor necrosis factor antagonist which prevents inflammatory response in joints, can give with methotrexate (DMARDs I) drug for an enhanced effect

DMARDs II side and adverse effects
Patients on these drugs are susceptible to infections, tumor necrosis factor helps fight against infections so when its suppressed it can make patients susceptible to infections. Heart failure, reactivation of latent TB can occur or new development of TB, severe skin reactions (such as Steven-johnsons syndrome, toxic epidermal necrolysis, erythema multiforme).

DMARDs II DRUG interventions
Monitor for skin reactions, assess for infection prior to each injection, signs and symptoms of infection during therapy, signs and symptoms of heart failure (cough, shortness of breath, elevated BP, elevated heart rate, pink Sputum), test for TB prior and during therapy because of risk of reoccurrence or new TB case

DMARD II administration
Give entanercept (Embrel) by sub Q and give twice a week, monitor site for redness, pain, and swelling after administration

DMARDs II patient instructions
Patients need to report signs and symptoms of infection, skin rashes, injection site reaction that doesn’t subside in a few days. Avoid unnecessary immunizations especially vaccinations with live vaccine because if possible virus transfer to patient

DMARD II contraindications
Patients with active infections, hematologic disease, malignancy

DMARDs II precautions
Not appropriate for people who have a autoimmune demyelinating disorder such as MS, avoid live vaccines

DMARDs II interactions
Taking DMARDs II drug and these chemotherapeutic drugs may cause bone marrow suppression (azathioprine, cyclophosphamide, methotrexate), do not give entanercept with anakinra (Kineret) because of risk of infections

Don’t treat RA frequently anymore. This is because of decreased side effects etc of DMARDs I AND II drugs. Gold sodium thiomalate (Aurolate) a form of gold salt was used to treat RA. Cytotoxic drugs that no longer used to treat RA are penicillamine (Cuprimine), azathioprine (Imuran), cyclosporine (sandinmune). Only used in severe RA cases

4 main types of drugs to treat osteoporosis
SERMs, Bisphosphonates, calcitonin, calcium supplements

Selective Estrogen Receptor Modulators SERMs used for
Used for prevention and treatment of postmenopausal osteoporosis, reduce risk of estrogen-dependent or receptor-positive breast cancer

SERMs prototype drug
raloxifene (evista), used more often because it poses less risk of uterine cancer

Tamoxifen (Nolvadex)
First SERMs drug but not used as often as raloxifene (Evista). Pregnancy D drug

raloxifene (Evista)
SERMS prototype drug used most often for osteoporosis treatment (poses less risk of uterine cancer). Pregnancy X drug

Expected pharmacologic action of SERMs
Activating estrogen receptors in endometrial tissue and bones. This activation decreases bone reabsorption, decreased bone loss. In contrast SERMs block access to estrogen receptors in breast tissue making them valuable drugs for patients with estrogen dependent or positive cancer

SERMs side effects, and adverse effects
Relate primarily to the activation of estrogen receptors. Serious adverse reactions to taking raloxifene are: increased risk of pulmonary embolism, deep vein thrombosis. Hot flashes, PREGNANCY CATAGORY X drug and can pass through breast milk

Raloxifene (Evista) serious adverse effects
Pulmonary emboli, DVT, PREGNANCY X drug, hot flashes

SERMs interventions
Monitor for thromboemboli in lower legs or lungs, monitor bone density

SERMs administration
Take with or without food, administer orally and daily.

SERMs patient instructions
Encourage patients to: consume adequate amount of calcium and vitamin D, use contraception and do not breastfeed during treatment, perform daily weight bearing exercises (walking, running), hot flashes may occur

SERMs contraindications
Pregnancy and breastfeeding, current or past history of DVT.

SERMs precautions
Use cautiously with patients with elevated serum lipid levels (hyperlipidemia) or on estrogen therapy

SERMs interactions
Because of the increased risk of estrogen supported cancers concurrent administration with estrogen is not recommended

Biphosphonates uses
Used for prevention and treatment of postmenopausal osteoporosis in women, age related osteoporosis in men, glucocorticoid-related osteoporosis

alendronate (Fosamax)
Prototype drug for Bisphosphonates

Other Bisphosphonates
Risedronate (actonel), Ibandronate (Boniva)

Risedronate (Actonel)
A Bisphosphonate drug

Ibandronate (Boniva)
A Bisphosphonate drug

Expected pharmacologic action of Bisphosphonates
Decrease bone resorption, decreases number and action of osteoclasts

Bisphosphonates side and adverse effects
Esophagitis, gastrointestinal disturbances such as (nausea, vomiting, abdominal pain), muscle and joint pain, eye pain and vision changes

Bisphosphonates interventions
Monitor for decreased bone absorption to determine the effectiveness of the therapy, if patients experience muscle and joint pain notify care provider to see if it can be managed with analgesics instead of a Bisphosphonate, monitor for changes in vision, watch for signs of esophagitis from not taking Bisphosphonates correctly

Bisphosphonates administration
Give 30 minutes before breakfast, give drug with full glass of water to prevent esophagitis, for 30 min after administration place patient in a sitting or standing position, make sure they avoid eating or drinking anything other then water during that time. Give mild analgesic for muscle and joint pain

Bisphosphonates patient instructions
Same guidelines as drug administration advise patient to take drug with full glass of water, to sit or stand for 30 minutes after taking the drug, report if pain persists, report changes in vision.

Restrictions are don’t eat or drink anything anything other then water 30 min after taking, don’t take calcium supplements or antacids 30 minutes after taking drug

Bisphosphonates contraindications
In patients with esophageal strictures/disorders or difficulty swallowing, do not give to patients unable to sit or stand for 30 min after administration, renal insufficiency, hypocalcemia

Bisphosphonates precautions
Take caution in patients with upper gastrointestinal disorders, infection, liver disease, heart failure

Bisphosphonates interactions
Calcium supplements and dairy products decrease absorption, do not give them within 30 min of administration of Bisphosphonates

Calcitonin use
Cannot prevent osteoporosis like SERMs, calcium supplements, or Bisphosphonates.
Calcitonin is used to treat of established postmenopausal osteoporosis, hypercalcemia secondary to hyperparathyroidism, Paget’s disease

Calcitonin prototype
The prototype and only drug in this catagory is calcitonin-salmon (Maicalcin). Administered sub q, intranasally, intramuscularly

Expected pharmacologic action of calcitonin
Decrease bone resorption, inhibit action of osteoclasts, increase excretion of calcium, decrease serum calcium in patients with hypercalcemia

Calcitonin side and adverse effects
Hypersensitivity reactions and anaphylaxis can occur in patients with a sketchy to fish proton of salmon, because calcitonin increases renal secretion of calcium hypocalcemia can occur if excretion exceeds intake, patients taking the nasal form of calcitonin may experience nasal dryness and irritation, may decrease in therapeutic effects if they take calcitonin over a long period of time

Calcitonin interventions
Assess nostrils for people using calcitonin nasally, monitor for symptoms of hypocalcemia such as muscle spasm, tingling of the fingers and toes, and serum calcium levels below the expected reference range, provide a high diet in calcium
And vitimin d, perform an intradermal allergy test prior to therapy. Watch for allergies to fish

Calcitonin administration
When administrating the nasal form of calcitonin: hold the nasal pump upright, prime the pump when using it the first time, spray once in nostril and alternate nostrils daily. When administrating sub q or intramuscular injections either salmon or human derived be sure to: rotate injection sites, protect from light (parenteral calcitonin), keep in fridge

Calcitonin patient instructions
Tell patients that use calcitonin intranasally to prime pump first use, alternate nostrils daily, report nasal irritation or bleeding. Instruct patients to notify provider of rash, itching, muscle spasm, tingling of fingers and toes, eat diet high in calcium and vitimin d, monitor for loss of effect after a year or more of use.

Calcitonin contraindications and precautions
Contraindication is allergy to salmon. And precaution is renal insufficiency

Calcitonin interactions
May decrease serum lithium levels

Calcium supplements uses
Treat Hypocalcemia, patients at risk for calcium deficiency such as adolescents, women who are pregnant, breastfeeding or postmenopausal, men or women at risk for osteoporosis, gastric hyperacidity

Calcium supplements prototype drugs
Calcium citrate (Citracel), Calcium carbonate (Tums)

Calcium citrate (Citracel)
Calcium supplement prototype drug, use primarily for calcium replacement.

Calcium carbonate (Tums)
Calcium supplement prototype drug, can use as a calcium supplement but primary used as an antacid

Expected pharmacologic action of calcium supplements
Expected to provide a non-dietary source of calcium, calcium is a base chemical so it’s affective in neutralizing gastric acid, calcium based antacids as calcium supplements, vitimin d is often used along side to enhance absorption of calcium from the intestine

Calcium supplements side and adverse effects
Risk for hypercalcemia (nausea, vomiting, constipation, increased utube output (polyuria), depression), kidney stones

Hypercalcemia signs and symptoms
Nausea, vomiting, constipation, increased urine output (polyuria) depression

Calcium supplements interventions
Periodically check serum calcium, monitor for signs of decreased gastric and intestinal motility (such as nausea, vomiting, constipation), monitor urine output in excess of intake, monitor for pain, monitor for blood in urine

Calcium supplements administration
Give calcium supplements 1 hour before or 1 to 2 hrs after glucocorticoids, thyroid supplements, tetracycline and quinolone antibiotics, give calcium based antacids 1 hour after meals and at bedtime with a full glass of water to increase solubility of the drug. Same process at bedtime

Calcium supplements patients instructions
Teach signs and symptoms of hypercalcemia, encourage high fiber diet, take laxatives and softener a as needed, take antacids 1 hour after meals and at bedtime, teach then to chew tablet before swallowing, drink water after swallowing, don’t take more then 600 mil grams at one time because the body can’t absorb more than that and will just excrete it, check label for the bioavailability of calcium in product, calcium citrate has a higher bioavailability than calcium carbonate because it is highly soluable. Calcium preparations a patient can chew also provide a higher bioavailability of the elemental calcium.

Calcium supplement contraindications
Hypercalcemia, low phosphate level (patients who have a low phosphate level can experiance an even greater decrease if you give them supplemental calcium due to the inverse relationship between calcium and phosphorus in the body, kidney stones, cardiac dysrhythmias.

Calcium supplements precautions
Give them with caution to people with low gastric molility

Calcium supplement interactions
Glucocorticoids decrease absorption of calcium, so don’t give at same time, calcium decreases absorption of thyroid hormones, tetracycline antibiotics, quinolone antibiotics. Thiazide diuretics decrease excretion of calcium. Food interactions are spinach, Swiss chard, whole grain breads, and cereal decrease absorption of calcium

Cholinesterase inhibitors uses
Used for treatment of myasthenia Gravis, improves muscle strength, improves endurance, give to promote muscle contractions

Cholinesterase inhibitor prototype drugs
Neostigmine (Prostigmin), Pyridostigmine (mestinon)

Edrophonium (tensilon)
Cholinesterase inhibitor that has a short duration of action which makes it useful in diagnosing myasthenia Gravis but not for treatment

Expected pharmacologic action of Cholinesterase inhibitors are
Prolong action of acetylcholine by inhibiting acetylcholineesterase, allow stronger and longer muscle contractions

Cholinesterase inhibitors side and adverse effects
Signs a serum level is to high is: increased intestinal motility, increased salivation, bradycardia, muscle weakness and respiratory paralysis (within 1 hour of admin)
Signs that serum levels are to low: Muscle weakness and respiratory paralysis (3 or more hours after admin)

Cholinesterase inhibitor interventions
Monitor for signs of toxicity which are: excessive diarrhea and or salivation. Check vital signs at beginning of therapy. Notify provider if apical pulse is below 60 beats per min, give 45 to 60 min prior to meals, have atropine ready to treat muscle weakness and respiratory paralysis that occurs 1 hour of admin. Assess ability to swallow before giving and that they can chew and swallow before eating food

Cholinesterase inhibitor admin
Give with a small amount of food 45 min to 1 hour before a meal to help strengthen the muscles used for chewing food. Develop a regular daily schedule that maintains the drug at therapeutic levels, if patients experience periods of weakness adjust admin schedule so you can consistently maintain the serum level at a therapeutic level.

Cholinesterase inhibitor patient instructions
Notify provider if patient experiance excessive diarrhea, muscle weakness, respiratory depression, or excessive salivation (could indicate toxicity). Teach patients how to take their pulse and notify if below 60 beats per min, eat meals within 45 min to 1 hour after taking drug, adjust schedule if periods of weakness are experienced, take drug at same time every day

Cholinesterase inhibitor contraindications
Patients who have a mechanical obstruction of the bowel or urinary tract

Cholinesterase inhibitor precautions
Be cautious with seizure disorders hyperthyroidism, peptic ulcer disease, asthma.

Cholinesterase inhibitor interactions
Since neuromuscular blocking agents and Cholinesterase inhibitors have opposite effects concurrent admin is a interaction you need to be aware of, neuromuscular blocking agents interfere with the actions of Cholinesterase inhibitors, Cholinesterase inhibitors DECREASE effects of nondepolarizing neuromuscular blocking agents, Cholinesterase inhibitors ENHANCE effects of depolarizing neuromuscular blocking agents

Neuromuscular blocking agents purpose
Given to inhibit muscle contraction /muscle paralysis

Neuromuscular blocking agent prototype/other drugs
Succinylcholine (Anectine), which is depolarizing, Pancurium, nondepolarizing.

Neuromuscular blocking agent pharmacologic action
Block action of acetylcholine at neuromuscular site causing muscle contraction to stop/paralysis

Neuromuscular blocking agents adverse/side effects
Muscle pain, hyperkalemia, hypotension, bradycardia, cardiac arrest, (specific adverse effect to succinylcholine is risk of malignant hyperthermia).

Neuromuscular blocking agents interventions
Monitor: potassium levels, take bp (watch for low), neck or back pain, cardiac/respiratory continuously.

Neuromuscular blocking agent contraindications/precautions
Contraindicated in patients with hyperkalemia (major burns, trauma), precautions with electrolyte imbalance, respiratory depression, and myasthenia Gravis

Neuromuscular blocking agent interactions
Cholinesterase inhibitors decrease the effects of non-polarizing neuromuscular blocking agents, and Cholinesterase inhibitors enhance the effects of demoralizing blocking agents. Both non and depolarizing neuromuscular blocking agents enhance the effects if aminoglycosides and tetracycline antibiotics

DMARDs I Drug used for rheumatoid arthritis

Paget’s disease
Paget disease is a localized disorder of bone remodeling that typically begins with excessive bone resorption followed by an increase in bone formation. This osteoclastic overactivity followed by compensatory osteoblastic activity leads to a structurally disorganized mosaic of bone (woven bone), which is mechanically weaker, larger, less compact, more vascular, and more susceptible to fracture than normal adult lamellar bone.

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