Drugs Acting on

Nutrition, Pain,
and Inflammation
Instructor:
Christine M. Fiel, RN MN LPT MAED
 Drugs Acting on Nutrition,
Pain, and Inflammation

a. Vitamins
b. Electrolytes
c. Analgesics (Opioid/Non-opioid)
d. Anti-inflammatory agents
Vitamins

-organic chemicals that are necessary for normal

metabolic functions and for tissue growth and
healing.
-The body needs only a small amount of vitamins
daily, which can be obtained through one’s diet.
-A well-balanced diet has all of the vitamins and
minerals needed for body functioning.
Vitamins
increased intake of vitamins :
• those experiencing periods of rapid body
growth
• pregnant or breastfeeding,
• those with debilitating illness
• those with malabsorptive issues (e.g.,
Crohn’s disease)
• those with inadequate diets (e.g.,
alcoholics, some geriatric patients).
• malnourished
Vitamins

• Vitamin deficiencies can cause cellular and

organ dysfunction that may result in slow
recovery from illness.
• Megadoses of vitamins are available,
advertised for specific health conditions; these
high doses can be toxic. Patients should be
advised to contact their health care provider
before taking these products.
 Vitamins

two general categories:

• fat-soluble
• water-soluble
Fat-soluble Vitamins
Vitamin A
 Fat-soluble Vitamins
Vitamin A
-essential for bone growth and the
maintenance of epithelial tissues, skin, eyes,
and hair
-used for the treatment of skin disorders such
as acne; -excess doses can be toxic
-During pregnancy, excessive amounts of
vitamin A (>6000 international units) might
have a teratogenic effect (birth defects) on
the fetus.
 Fat-soluble Vitamins
Vitamin A
Pharmacokinetics: When a person is deficient
in vitamin A, the vitamin is absorbed faster
than when there is no deficiency or intestinal
obstruction. A portion of vitamin A is stored in
the liver, and this function can be inhibited
with liver disease. Massive doses of vitamin A
may cause hypervitaminosis A, symptoms of
which are hair loss, peeling skin, anorexia,
abdominal pain, lethargy, nausea, and
vomiting.
 Fat-soluble Vitamins
Vitamin A
Pharmacodynamics: Vitamin A is necessary
for many biochemical processes. It aids in the
formation of the visual pigment needed for
night vision. This vitamin is needed in bone
growth and development, and it promotes the
integrity of the mucosal and epithelial tissues.
An early sign of vitamin A deficiency
(hypovitaminosis A) is night blindness. This
may progress to dryness and ulceration of the
cornea and to blindness.
Vitamin D
 Fat-soluble Vitamins
Vitamin D
-has a major role in regulating calcium and
phosphorus metabolism and is needed for
calcium absorption from the intestines
-Dietary vit. D is absorbed in the small intestine
and requires bile salts for absorption.
-two compounds of vit. D:
• vitamin D2, ergocalciferol (a synthetic fortified
vitamin D),
• vitamin D3, cholecalciferol (a natural form of
vitamin D influenced by ultraviolet sunlight
through the skin).
 Fat-soluble Vitamins
Vitamin D
-Over-the-counter vit. D supplements usually
contain vitamin D3.
-Once absorbed, vitamin D is converted to
calcifediol (also known as 25
hydroxycholecalciferol) in the liver.
-Calcifediol is then converted to an active
form, calcitriol, in the kidneys.
-Studies have suggested that vitamin D, taken
with calcium, can reduce the incidence of
fractures.
 Fat-soluble Vitamins
Vitamin D
-Excretion of vitamin D is primarily in bile; only
a small amount is excreted in the urine
-Excess vitamin D ingestion (>40,000
international units) results in hypervitaminosis D
and may cause hypercalcemia (an elevated
serum calcium level).
-Anorexia, nausea, and vomiting are early
symptoms of vitamin D toxicity.
Vitamin E
 Fat-soluble Vitamins
Vitamin E
-has antioxidant properties that protect
cellular components from being oxidized and
red blood cells from hemolysis
-depends on bile salts, pancreatic secretion,
and fat for its absorption
-Vitamin E is stored in all tissues, especially the
liver, muscle, and fatty tissue
-About 75% of vitamin E is excreted in bile.
 Fat-soluble Vitamins
Vitamin E
-taking 400 to 800 IU of vit. E per day reduces the
number of nonfatal myocardial infarctions (MIs)
-taking 200 IU per day for several years can reduce
the risk of coronary artery disease (CAD), but the use
of vitamin E for CAD is being questioned.
-many still state that this vitamin protects the heart
and arteries
-aids in the prevention of macular degeneration
because of its antioxidant effects
-Many patients with Alzheimer’s or Parkinson’s disease
take supplemental vit. E for its antioxidant effects.
 Fat-soluble Vitamins
Vitamin E
-Side effects of large doses of vitamin E may
include fatigue, weakness, nausea, GI upset,
headache, and breast tenderness. Vitamin E
may prolong the prothrombin time (PT).
-Patients taking warfarin should have their PT
monitored closely.
-Iron and vitamin E should not be taken
together because iron can interfere with the
body’s absorption and use of vitamin E.
Vitamin K
 Fat-soluble Vitamins
Vitamin K
-occurs in four forms:
1. Vitamin K1 (phytonadione) is the most active form;
2. vitamin K2 (menaquinone) is synthesized by
intestinal flora;
3. vitamin K3 (menadione) and
4. vitamin K4 (menadiol) have been produced
synthetically.

Vitamin K2 is not commercially available. Vitamins K1

and K2 are absorbed in the presence of bile salts.
Vitamins K3 and K4 do not need bile salts for
absorption. After vitamin K is absorbed, it is stored
primarily in the liver and in other tissues. Half of vitamin
K comes from the intestinal flora, and the remaining
portion comes from one’s diet.
 Fat-soluble Vitamins
Vitamin K
-needed for synthesis of prothrombin and the
clotting factors VII, IX, and X.
-vitamin K1 (phytonadione) is the only vitamin K
form available for therapeutic use and is most
effective in preventing hemorrhage.
The commercial drugs available for vitamin K1 are
called Mephyton and AquaMEPHYTON.
Vitamin K is used for two reasons:
(1) as an antidote for oral anticoagulant overdose
(2) to prevent and treat the hypoprothrombinemia
of vitamin K deficiency.
 Fat-soluble Vitamins
Vitamin K
-Spontaneous hemorrhage may occur with
vitamin K deficiency due to lack of bile salts and
malabsorption syndromes that interfere with
vitamin K uptake (e.g., celiac disease).
-Newborns are vitamin K deficient; thus, a single
dose of phytonadione is recommended
immediately after delivery. This practice is
common in the United States but controversial in
other countries. This can elevate the bilirubin level
and cause hyperbilirubinemia with a risk of
kernicterus. There are oral and parenteral forms of
phytonadione; IV administration is dangerous and
may cause death.
Water-Soluble Vitamins
 Water-Soluble Vitamins
Vitamin B Complex
- common group of vitamins administered in the
clinical setting, especially to patients with
alcoholism.
 Water-Soluble Vitamins
Vitamin B1:
Thiamine deficiency can lead to the polyneuritis
and cardiac pathology seen in beriberi or to
Wernicke’s encephalopathy that progresses to
Korsakoff’s syndrome, conditions most commonly
associated with alcohol abuse.
Wernicke-Korsakoff syndrome:
-a significant CNS disorder characterized by
confusion, nystagmus, diplopia, ataxia, and loss of
recent memory.
-If not treated, it may cause irreversible brain
damage.
-IV administration of thiamine is recommended for
treatment
-Thiamine must be given before giving any glucose
to avoid aggravation of symptoms.
 Water-Soluble Vitamins
Vitamin B2:

-Riboflavin may be given for:

• scaly dermatitis
• cracked corners of the mouth
• inflammation of the skin and tongue

-To treat migraine headache, riboflavin is given

in larger doses than for dermatologic concerns.
 Water-Soluble Vitamins
Vitamin B3:

-Niacin is given to alleviate pellagra and

hyperlipidemia, for which large doses are
required.

-However, large doses may cause GI irritation

and vasodilation, resulting in a flushing
sensation.
 Water-Soluble Vitamins
Vitamin B6:
-Pyridoxine is administered to correct vitamin B6
deficiency and help alleviate the symptoms of
neuritis caused by isoniazid (INH) therapy for
tuberculosis.
-an essential building block of nucleic acids, red
blood cell formation, and synthesis of hemoglobin. -
used to treat neonates with seizures refractive to
traditional therapy.
-Vit. B6 deficiencies may occur in alcoholics along
with deficiencies of other B-complex vitamins.
-Patients with diabetes or alcoholism may benefit
from daily supplementation.
-Pyridoxine is readily absorbed in the jejunum and
stored in the liver, muscle, and brain. It is
metabolized in the liver and excreted in the urine.
 Water-Soluble Vitamins
Vitamin C (ascorbic acid)
- recommended daily
dose of vitamin C for
an adult is 50 to 100
mg/day

Increased amounts:
-treat URTI, cancer, or
hypercholesterolemia.

-Massive doses of vitamin C

can cause diarrhea and GI
upset.
 Water-Soluble Vitamins
Vitamin C (ascorbic acid)
Pharmacokinetics: Vit. C is absorbed readily
through the GI tract and is distributed throughout
the body fluids. The kidneys completely excrete
vitamin C, mostly unchanged.

Pharmacodynamics: Vit. C is needed for

carbohydrate metabolism and protein and lipid
synthesis. Collagen synthesis also requires vitamin C
for capillary endothelium, connective tissue and
tissue repair, and osteoid tissue of the bone. Large
doses of vitamin C (>5 to 10 g) may decrease the
effect of oral anticoagulants. Smoking decreases
serum vitamin C levels.
-Vitamin C (in doses >500 mg) aids iron absorption.
 Water-Soluble Vitamins
Vitamin C (ascorbic acid)
-Most authorities believe that vitamin C does not
cure or prevent the common cold; rather, they
believe that vitamin C has a placebo effect.
-Moreover, megadoses of vitamin C taken with
aspirin or sulfonamides may cause crystal
formation in the urine (crystalluria).
-Excessive doses of vitamin C can cause a false-
negative occult (blood) stool result and false-
positive sugar result in the urine.
-If large doses of megavitamins are to be
discontinued, a gradual reduction of dosage is
necessary to avoid vitamin deficiency.
 Water-Soluble
Vitamins
Vitamin B9 (folic acid/folate)
- absorbed from the
small intestine, and the
active form of folic
acid (folate) is
circulated to all tissues.
- One third of folate is
stored in the liver, and
the rest is stored in
tissues.
- -80% of folate is
excreted in bile and
20% in urine.
 Water-Soluble Vitamins
Vitamin B9 (folic acid/folate)
- essential for body growth
- needed for DNA synthesis
- without folic acid there is a disruption in cellular
division
Causes of deficiency:
- Chronic alcoholism, poor nutritional intake,
malabsorption syndromes, pregnancy, and drugs
that cause inadequate absorption (phenytoin,
barbiturates) or folic acid antagonists (methotrexate,
triamterene, trimethoprim)
Symptoms: anorexia, nausea, stomatitis, diarrhea,
fatigue, alopecia, and blood dyscrasias (megaloblastic
anemia, leukopenia, thrombocytopenia).

These symptoms are usually not noted until 2 to 4

months after folic acid storage is depleted.
 Water-Soluble Vitamins
Vitamin B9 (folic acid/folate)
- Excessive doses of folic acid may mask signs
of vitamin B12 deficiency, which is a risk in
older adults.
- Patients taking phenytoin (Dilantin) to control
seizures should be cautious about taking folic
acid. This vitamin can lower the serum
phenytoin level, which could increase the risk
of seizures. The phenytoin dose would need
to be adjusted in such patients.
 Water-Soluble
Vitamins
Vitamin B12 (Cobalamin)
- essential for DNA
synthesis
- aids in the conversion of
folic acid to its active
form, With active folic
acid, vitamin B12
promotes cellular division
- needed for normal
hematopoiesis and to
maintain nervous system
integrity, especially the
myelin.
 Water-Soluble Vitamins
Vitamin B12 (Cobalamin)
Intrinsic factor:
-produced by gastric parietal cells
- necessary for the absorption of vitamin B12
through the intestinal wall
- After absorption, vitamin B12 binds to the protein
transcobalamin II and is transferred to the tissues.
- Most vitamin B12 is stored in the liver.
- Vitamin B12 is slowly excreted, and it can take 2
to 3 years for stored vitamin B12 to be depleted
and a deficit noticed.
 Water-Soluble Vitamins
Vitamin B12 (Cobalamin)

-deficiency is uncommon unless there is a

disturbance of the intrinsic factor and intestinal
absorption
-Pernicious anemia (lack of the intrinsic factor) is
the major cause of vitamin B12 deficiency.
-Vitamin B12 deficiency can also develop in
strict vegetarians who do not consume meat,
fish, or dairy products.
 Water-Soluble Vitamins
Vitamin B12 (Cobalamin)
-Other possible causes of deficiency include
malabsorption syndromes (cancer, celiac disease,
certain drugs), gastrectomy, Crohn’s disease, and
liver and kidney diseases.
-B12 deficiency is commonly seen with metformin
and proton pump inhibitors (e.g., omeprazole).

Symptoms: numbness and tingling in the lower

extremities, weakness, fatigue, anorexia, loss of
taste, diarrhea, memory loss, mood changes,
dementia, psychosis, megaloblastic anemia with
macrocytes (overenlarged erythrocytes [red blood
cells]) in the blood, and megaloblasts
(overenlarged erythroblasts) in the bone marrow.
 Water-Soluble Vitamins
Vitamin B12 (Cobalamin)

-To correct vitamin B12 deficiency,

cyanocobalamin in crystalline form can be
given intramuscularly for severe deficits.
-It cannot be given intravenously because of
possible hypersensitive reactions.
-Cyanocobalamin can be given orally and is
commonly found in multivitamin preparations. It
can also be given as a subcutaneous injection.
Minerals
 Iron
Iron (ferrous sulfate, gluconate, or fumarate) is
vital for hemoglobin regeneration.
-Sixty percent of the iron in the body is found in
hemoglobin.
-One of the causes of anemia is iron deficiency.
-A normal diet contains 5 to 20 mg of iron per
day.
-Foods rich in iron include liver, lean meats, egg
yolks, dried beans, green vegetables (e.g.,
spinach), and fruit.
-Food and antacids slow the absorption of iron,
and vitamin C increases iron absorption.
 Iron
-During pregnancy, an increased amount of iron is
needed, but during the first trimester of pregnancy
megadoses of iron are contraindicated because of
its possible teratogenic effect on the fetus.
-Larger doses of iron are required during the second
and third trimesters of pregnancy.
-The dose of iron for infants and children 6 months to
2 years of age is 1.5 mg/kg of body weight. For the
adult, 50 mg/ day is needed for hemoglobin
regeneration. The ferrous sulfate tablet is 325 mg, of
which 65 mg is elemental iron.
-Therefore one tablet of ferrous sulfate is sufficient as
a daily iron dose when indicated.
 Copper
-needed for the formation of RBCs and
connective tissues
-It is a cofactor of many enzymes, and its function
is in the production of the neurotransmitters
norepinephrine and dopamine.
-Excess serum copper levels may be associated
with Wilson’s disease, which is an inborn error of
metabolism that allows for large amounts of
copper to accumulate in the liver, brain, cornea
or kidneys.
 Copper
-A prolonged copper deficiency may result in
anemia, which is not corrected by taking iron
supplements.
-Abnormal blood and skin changes caused by a
copper deficiency include a decrease in white
blood cell count, glucose intolerance, and a
decrease in skin and hair pigmentation.
-Mental retardation may also occur in the young.
-The RDA for copper is 1.5 to 3 mg/day.
-Most adults consume about 1 mg/day. Foods
rich in copper are shellfish (crab, oysters), liver,
nuts, seeds (sunflower, sesame), legumes, and
cocoa.
 Zinc
-Zinc is important to many enzymatic reactions
and is essential for normal growth and tissue
repair, wound healing, and taste and smell.
-The use of zinc has greatly increased in the past
few years; some believe zinc can alleviate
symptoms of the common cold and shorten its
duration.
-Individuals may take as much as 200 mg/day.
-The adult RDA is 12 to 19 mg/ day.
-Foods rich in zinc include beef, lamb, eggs, and
leafy and root vegetables.
 Zinc
-Large doses, more than 150 mg, may cause a
copper deficiency, a decrease in high-density
lipoprotein (HDL) cholesterol (“good”
cholesterol), and a weakened immune response.
-Zinc can inhibit tetracycline absorption.
-Patients taking zinc and an antibiotic should not
take them together; zinc should be taken at least
2 hours after taking an antibiotic.
-Patients on long-term parenteral nutrition are at
risk for zinc deficiency.
-Serum zinc levels may not correlate with degree
of deficiency.
 Chromium
-helpful in the control of type 2 diabetes (non–
insulin-dependent diabetes)
-helps to normalize blood glucose by increasing
the effects of insulin on the cells
-If a patient is taking large doses of chromium and
an oral hypoglycemic agent or insulin, the
glucose level should be monitored closely for a
hypoglycemic reaction.
-Some patients with an impaired glucose
tolerance or patients who do not have diabetes
may benefit by taking chromium.
-claims to promote weight loss and muscle
building
 Chromium
There is no RDA for chromium; however,
50 to 200 mcg/ day is considered within
the normal range for adults and children
older than 6 years of age.

Foods rich in chromium include meats,

whole-grain cereals, and brewer’s yeast.
 Selenium
-acts as a cofactor for an antioxidant enzyme
that protects protein and nucleic acids from
oxidative damage
-Selenium works with vitamin E.
-It is thought that selenium has an anti-
carcinogenic effect, and doses lower than
200 mcg may reduce the risk of lung, prostate,
and colorectal cancer.
-Excess doses of more than 200 mcg might
cause weakness, hair loss, dermatitis, nausea,
diarrhea, and abdominal pain. Also, there
may be a garlic-like odor from the skin and
breath.
 Selenium
The RDA for selenium is 40 to 75
mcg (lower dose for women, higher
dose for men).

Foods rich in selenium include

meats (especially liver), seafood,
eggs, and dairy products.
 Pain and
Inflammation
Management
Agents
• Inflammation is a reaction to tissue injury
caused by the release of chemical
mediators that trigger both a vascular
response and the migration of fluid and cells
(leukocytes, or white blood cells) to the
injured site.

The chemical mediators are:

1. Histamines
2. kinins
3. prostaglandins
• Histamine, the first mediator in the
inflammatory process, causes dilation
of the arterioles and increases capillary
permeability, allowing fluid to leave
the capillaries and flow into the injured
area.
• Kinins, such as bradykinin, also
increase capillary permeability and
the sensation of pain.
• Prostaglandins are released, causing
an increase in vasodilation, capillary
permeability, pain, and fever.
• Inflammation:
-may or may not be the result of an
infection;
-only a small percentage of
inflammations are caused by infections.
-Other causes of inflammation include
trauma, surgical interventions, extreme
heat or cold, and caustic chemical
agents.
Infection is caused by microorganisms
and results in inflammation, but not all
inflammations are caused by infections.

Cardinal Signs of Inflammation:

1. Redness
2. Swelling (edema)
3. Heat
4. Pain
5. Loss of function
• Cyclooxygenase (COX) is the enzyme
responsible for converting arachidonic acid
into prostaglandins and their products.
• This synthesis of prostaglandins causes
inflammation and pain at a tissue injury site.

There are two enzyme forms of cyclooxygenase:

a. COX-1: protects the stomach lining and
regulates blood platelets
b. COX-2: triggers inflammation and pain
 TWO PHASES OF
INFLAMMATION
1. Vascular Phase:
-occurs 10 to 15 minutes after an injury
-associated with vasodilation and increased
capillary permeability, during which blood
substances and fluid leave the plasma and go
to the injured site.

2. Delayed Phase:
-occurs when leukocytes infiltrate the inflamed
tissue.
ANTIINFLAMMATORY AGENTS
• Aspirin inhibit the biosynthesis of prostaglandin and
are therefore called prostaglandin inhibitors.
• Because prostaglandin inhibitors affect the
inflammatory process, they are more commonly
called antiinflammatory agents.
Antiinflammatory agents also:
-relieve pain (analgesic)
-reduce elevated body temperature (antipyretic)
-inhibit platelet aggregation (anticoagulant)
Nonsteroidal Antiinflammatory Drugs (NSAIDs)
-Most NSAIDs are used to decrease inflammation and
pain for patients who have some type of arthritic
condition.
 NONSTEROIDAL
ANTIINFLAMMATORY DRUGS
• NSAIDs
-aspirin and aspirin-like drugs that inhibit the enzyme COX,
which is needed for the biosynthesis of
prostaglandins
- may be called prostaglandin inhibitors with varying
degrees of analgesic and antipyretic effects
- used primarily as antiinflammatory agents to relieve
inflammation and pain
- Their antipyretic effect is less than their antiinflammatory
effect.
- Not suggested for use in alleviating mild headaches and
mildly elevated temperature
Groups of NSAIDs:
1. Salicylates
2. Para-chlorobenzoic acid derivatives, or indoles
3. Phenylacetic acids
4. Propionic acid derivatives
5. Fenamates
6. Oxicams
7. Selective COX-2 (Cyclooxygenase) inhibitors

The first six NSAID groups on the list are known as first
generation NSAIDs, and the COX-2 inhibitors are
called second-generation NSAIDs.
 Salicylates

Aspirin
-also called acetylsalicylic acid (ASA)
-developed in 1899 by Adolph Bayer
-oldest antiinflammatory agent
-decreases the inflammatory process
-also considered an antiplatelet drug for patients with
cardiac or cerebrovascular disorders
-gastric distress is a common problem
-should not be taken with other NSAIDs because it
decreases the blood level and effectiveness of NSAIDs.
*Aspirin and other
NSAIDs relieve pain
by inhibiting the
enzyme COX, which
is needed for the
biosynthesis of
prostaglandins.

*New NSAIDs, called COX-2

inhibitors, block only COX-2
and not COX-1. These drugs
leave protection for the
stomach lining intact (no
gastric bleeding and ulcers),
but still deliver relief for pain
and inflammation.
 Para-Chlorobenzoic Acid
Indomethacin (Indocin)
-One of the first NSAIDs introduced
-used for rheumatoid arthritis, gouty arthritis, and
osteoarthritis
-a potent prostaglandin inhibitor
-highly protein bound (90%) and displaces other protein-
bound drugs, resulting in potential toxicity
-has a moderate half-life (4.5 hours)
-very irritating to the stomach and should be taken with
food
Two other para-chlorobenzoic acid derivatives:
-sulindac (Clinoril)
-tolmetin (Tolectin)
*both produce less severe adverse reactions than
indomethacin
*This group of NSAIDs may cause sodium and water
retention and increased blood pressure.
 Phenylacetic Acid Derivatives
Diclofenac sodium (Voltaren-XR)
- Has a plasma half-life of 1.2 to 2 hours
- analgesic and antiinflammatory effects are similar to
those of aspirin
- Has minimal to no antipyretic effects
- indicated for rheumatoid arthritis, osteoarthritis, and
ankylosing spondylitis
- available in PO, extended-release, and topical 1% gel
preparations
Ketorolac (Toradol)
- First injectable NSAID
- Inhibits prostaglandin synthesis
- has greater analgesic properties than other
antiinflammatory agents
- Recommended for short-term management of pain
- Postsurgical Pain: shown analgesic efficacy equal or
superior to that of opioid analgesics.
- IM in doses of 30-60 mg q6h for adults.
- available in PO, IV, and intranasal preparations.
 Propionic Acid Derivatives

-aspirin-like but have stronger effects and create less

GI irritation
-highly protein-bound better tolerated than other
NSAIDs
-Gastric upset occurs

Ibuprofen (Motrin)
- most widely used
 Fenamates
- Includes potent NSAIDs used for acute and chronic
arthritic conditions.
- Gastric irritation is a common side effect
- Patients with a history of peptic ulcer should avoid
taking this group of drugs.
- Other side effects: edema, dizziness, tinnitus, and
pruritus
- Two fenamates are meclofenamate sodium
monohydrate (Meclomen) and mefenamic acid
(Ponstel).
 Oxicams
Piroxicam (Feldene)
-indicated for long-term arthritic conditions such as
rheumatoid arthritis and osteoarthritis.
-can cause gastric problems: ulceration and
epigastric distress
-It is well tolerated, and its major advantage over
other NSAIDs is its long half-life, which allows it to be
taken only once daily.
-highly protein-bound
-should not be taken with aspirin or other NSAIDs
 Selective COX-2 Inhibitors
(Second-Generation NSAIDs)
• To decrease inflammation and pain
• Most NSAIDs are nonselective inhibitors that inhibit COX-1
and COX-2.
• By inhibiting COX-1, protection of the stomach lining is
decreased and clotting time is also decreased, which
may benefit the patient with cardiovascular or coronary
artery disease (CAD).
• Selective COX-2 inhibitors are drugs of choice for
patients with severe arthritic conditions who need high
doses of an antiinflammatory drug, because large doses
of NSAIDs may cause peptic ulcer and gastric bleeding.
• celecoxib (Celebrex): COX-2 inhibitor
• Nabumetone (Relafen): inhibits COX-2 more than COX-1
 DISEASE-MODIFYING
ANTIRHEUMATIC DRUGS
DMARDs

• immunosuppressive agents
• Immunomodulators
• antimalarials
 Immunosuppressive
Agents
-used to treat refractory rheumatoid arthritis (arthritis that
does not respond to antiinflammatory drugs).
-In low doses, selected immunosuppressive agents have
been effective in the treatment of rheumatoid arthritis.
-Drugs such as azathioprine (Imuran),
cyclophosphamide (Cytoxan), and methotrexate
(Mexate), primarily used to suppress cancer growth and
proliferation, might be used to suppress the inflammatory
process of rheumatoid arthritis when other treatments
fail.
-In one study of patients receiving cyclophosphamide,
few new erosions of joint cartilage were present,
suggesting that the disease process was not active.
 Immunomodulators
• Treat moderate to severe rheumatoid arthritis by
disrupting the inflammatory process and delaying
disease progression.
Classifications:
• Interleukin (IL-1) receptor antagonists:
-contributes to synovial inflammation and joint
destruction ex. Anakinra(Kineret)
• Tumor necrosis factor (TNF) blockers:
-bind to TNF and block it from attaching to TNF
receptors on synovial cell surfaces
ex. Etanercept (Enbrel) and Infliximab (Remicade)
 Antimalarials
• Used to treat rheumatoid arthritis when
other methods of treatment fail
• Effect may take 4 to 12 weeks to
become apparent
• antimalarials are usually used in
combination with NSAIDs in patients
whose arthritis is not under control
 ANTIGOUT DRUGS
• Gout is an inflammatory condition that attacks joints
tendons, and other tissues.
• It may be called gouty arthritis.
• The most common site of acute gouty inflammation
is at the joint of the big toe.
• Gout is characterized by a uric acid metabolism
disorder and a defect in purine (products of certain
proteins) metabolism, which results in an increase in
urates (uric acid salts) and an accumulation of uric
acid (hyperuricemia) or an ineffective clearance of
uric acid by the kidneys.
• Gout may appear as bumps, or tophi, in the
subcutaneous tissue of earlobes, elbows, hands,
and the base of the large toe.
 Antiinflammatory Gout
Drug: Colchicine
• First drug used to treat gout, 1936
• Inhibits the migration of leukocytes to the inflamed site.
• Effective in alleviating acute symptoms of gout, but it is
not effective in decreasing inflammation occurring in
other inflammatory disorders.
• Colchicine does not inhibit uric acid synthesis and does
not promote uric acid excretion. It should not be used if
the patient has a severe renal, cardiac, or GI
problem.
• Gastric irritation is a common problem, so colchicine
should be taken with food.
• With high doses, nausea, vomiting, diarrhea, or
abdominal pain occurs in approximately 75% of patients
taking the drug.
Uric Acid Inhibitor
 Uricosurics
• Increase the rate of uric acid excretion by
inhibiting its reabsorption
• Effective in alleviating chronic gout, but they
should not be used during acute attacks
• Probenecid (Benemid): 1945, blocks the
reabsorption of uric acid and promotes its
excretion
• Probenecid should be taken with meals.
• It has an average half-life of 8 to 10 hours and is
85% to 95% protein-bound.
• Use caution when administering this drug with
other highly protein-bound drugs.
Thank you!