Lesson 4: Anti-Inflammatory, Anti-Allergy, and

Immunologic Drugs

ACTIVE IMMUNIZATION

• consists of the administration of antigen

to the host to induce formation of
antibodies and cell-mediated immunity.

• DOWNSIDE: requires time to develop

and is therefore generally inactive at the
time of a specific exposure.

PASSIVE IMMUNIZATION

• consists of transfer of immunity to a host

using preformed immunologic products.

• Passive Immunization is useful for:

1. Individuals unable to form

antibodies.

Example: Congenital
Agammaglobulinemia

2. Prevention of disease when

time does not permit active
immunization.

Example: Post exposure

3. For treatment of certain

diseases normally prevented by
immunization.

Example: Tetanus

4. For treatment of conditions for

which active immunization is
unavailable or impractical.

Example: Snakebite
CHILDHOOD IMMUNIZATION
NOTE: sabi ni ma’am need daw tandaan tong 2: vaccine and it’s route.

VACCINE ROUTE
Diphtheria Tetanus Acellular Pertussis (DTaP) Intramuscular
Haemophilus Influenzae Type B Conjugate Intramuscular
Hepatitis A Intramuscular
Hepatitis B Intramuscular
Subcutaneous (ACCEPTABLE lang sa individuals with
BLEEDING disorders)
Human Papillomavirus (HPV) Intramuscular
Influenza, Inactivated Intramuscular
Intradermal (AVAILABLE lang kapag 18-64 years old)
Influenza, Live attenuated Intranasal
Measles - mumps- rubella (MMR) Subcutaneous
Meningococcal Conjugate Intramuscular
Meningococcal Polysaccharide Subcutaneous
Pneumococcal Conjugate Intramuscular or Subcutaneous
Pneumococcal Polysaccharide Intramuscular or Subcutaneous
Poliovirus Vaccine, Inactivated Subcutaneous
Rabies Intramuscular
Rotavirus Oral
Tetanus – Diphtheria (Td or DT) Intramuscular
Tetanus, Diphtheria Pertussis Intramuscular
Typhoid, Ty21 a oral Oral
Typhoid, Vi capsular Polysaccharides Intramuscular
Varicella Subcutaneous
Yellow Fever Subcutaneous
Zoster Subcutaneous

RECOMMENDED SCHEDULE

PASSIVE IMMUNIZATION
Note: additional information lang daw ito.
 CANCER CHEMOTHERAPY  The goal is to render the local
therapy more effective.
• Classifications of drugs:
3. ADJUVANT CHEMOTHERAPY
▪ Based on Cell cycle
 chemotherapy done AFTER local
• CELL CYCLE NONSPECIFIC DRUGS (CCNS) treatment procedures such as
▪ act on tumor stem cells when surgery or radiation.
they are traversing the cell cycle  reduce the risk of local and
and when they are in the resting systemic recurrence and to
phase. improve disease-free and
• CELL CYCLE SPECIFIC DRUGS (CCS) overall survival.

▪ act selectively on tumor stem CHEMOTHERAPY TOXICITIES

cells when they are traversing
the cell cycle, and not when they
are in the G0 phase.

Note:

• M – itosis Note:
• S – ynthesis
B: Bleomycin – Pulmonary Fibrosis (LUNGS)
CANCER TREATMENT MODALITIES
C: Cisplatin / Carboplatin – Nephrotoxicity &
1. PRIMARY INDUCTION CHEMOTHERAPY Acoustic nerve damage

 drug therapy is administered as D: Doxorubicin – Cardiotoxicity

the primary treatment.
M/F: Methotrexate, 5- Flurouracil -
2. NEOADJUVANT CHEMOTHERAPY Myelosupression

 use of chemotherapy in patients N: Nitrosoureas – Neurotoxic

with localized cancer BEFORE
P: Clycophosphamide – Hemorrghagic Cystitis
performing local therapy
(UTI na may dugo)
(surgery).
T: Taxanes – Peripheral Neuropathy
V: Vinca Alkdaloids – Peripheral Neuropathy
 ALKYLATING AGENTS

Note:

• Chronic lymphocytic leukemia – most common leukemia in adults.

ANTIMETABOLITES

Note:

• Methotrexate – antimetabolites mimic your purine and pyrimidines.

 Leucovorin – Rescue Therapy

Uses:

▪ Choriocarcinoma
▪ Arthritis

• 6- Mercaptopurine – a purine.
 antimetabolites mimic your purine and pyrimidines.

USES:
 ▪ Acute leukemia (AML, ALL)
• Pemetrexed - a purine.
 antimetabolites mimic your purine and pyrimidines.

USES:

▪ Mesothelioma
▪ Non-small lung cancer

• Cytarabine – a pyrimidine.
 MOST SPECIFIC for the 5 phases of Cell Cycle.

USES:

▪ Acute leukemia (AML, ALL)

▪ CML in blast cells

• 5-Flurouracil – a pyrimidine.

USES:

▪ Breast Cancer
▪ Colorectal
▪ Head and neck cancer

• Gemcitabine – a pyrimidine.

USES:

• Pancreatic Cancer

NATURAL PRODUCT ANTICANCER DRUGS

Note:

• Vincristine & Vinblastine – a vinca alkaloid.

 Prevents microtubule
 Acts primarily in M phase of cancer cell cycle

• Vincristine – DO NOT cause bone marrow.

• Vinblastine – cause bone marrow suppression

• Etoposide – a podophyllotoxin.
  Inhibits DNA topoisomerase.

• Topotecan – a camptothecan.
 Inhibits topoisomerase 1.

• Paclitaxel – interferes with mitotic spindle.

ANTI TUMOR DRUGS

Note:

• Doxorubicin – anthracycline.
 Dexrazoxane – rescue therapy.

• Bleomycin – antitumor antibiotic.

 MOST SPECIFIC for the G2 phase of the cell cycle.

• Actinomycin – antitumor antibiotic.

MISCELLANEOUS ANTICANCER DRUGS

Note:

• Imatinib – Tyrosine kinase inhibitors.

 Brand: Gleevec
 Preg cat class D

• Trastuzumab – Monoclonal antibody.

 Brand: Herceptin
 • Bevacizumab - Monoclonal antibody.
 Inhibits binding of VEGF to VEGFR leading to inhibition of VEGF signaling.
 Inhibits angiogenesis.
 BeVacizumab – for BLOOD VESSELS.

• Rituximab - Monoclonal antibody.

 CD20 inhibitor.

• Cetuximab – Monoclonal antibody.

 Binds to EGFR
 USED in Colorectal Cancer

• Erlotinib – EGFR TK inhibitor.

 Preg cat D

• Interferon-Alpha – Interferon.

• Asparaginase – Substrate depleting enzyme.

• All – trans retinoic acid – Vitamin A derivative.

HORMONAL ANTICANCER DRUGS

Notes:

• Prednisone – Glucocorticoid.
 Suppresses inflammation and immune response.

USES:

▪ Hodgkin lymphomas
▪ Chronic Lymphocytic Leukemia

• Tamoxifen – selective estrogen receptor modulator.

USES:

▪ Hormone sensitive breast cancer

• Flutamide – Androgen antagonist.

USES:

▪ Prostate cancer
▪ Surgical castration

• Leuprolide – GnRh analog.

• Anastrozole – Estrogen synthesis inhibitor.

 HITAMINERGIC • Should not be given to neonates because
they are more susceptible to
HISTAMINE
antimuscarinic effects.
• Formed from the amino acid histidine,
• Possess antimuscarinic, adrenaline-
metabolized by the enzyme’s
antagonizing, serotonin antagonizing,
monoamine oxidase and diamine
and local anaesthetic effects.
oxidase.
• Some have calcium-channel blocking
• Important pathophysiologic roles:
activity.
▪ Seasonal rhinitis (hay fever),
• All are PO but can be given topical (nose
urticaria, and angioedema.
and eyes)
▪ Control of acid secretion in the
• Negligible effect on H2 receptors
stomach.

TRIPLE RESPONSE OF LEWIS (WHEAL, FLUSH

AND FLARE)

• Classic demonstration of histamine

effect.

• Mediated mainly by h1 and h2

receptors.

• Involves a small red spot at the center of

an intradermal injection.

• Of histamine surrounded by a red

edematous wheal.

H1 RECEPTOR ANTAGONISTS

• Common SE: Sedation

 NON-STEROIDAL ANTI-INFLAMMATORY ▪ effective in reducing platelet
DRUGS aggregation.

General Classification of NSAIDs: ▪ follows first-order elimination

kinetics.
1. SALICYLATES
• Intermediate doses (300–2400 mg/d)
▪ Aspirin
▪ antipyretic and analgesic
2. NONSELECTIVE NSAIDs
effects.
▪ Ibuprofen, Indomethacin,
• High doses (2400–4000 mg/d)
Ketorolac, Piroxicam
▪ anti-inflammatory effects
3. COX-2 SELECTIVE
▪ follows zero-order elimination
▪ Celecoxib, Etoricoxib, Parecoxib
kinetics.
COMMON NSAID TOXICITIES
PARACETAMOL OVERDOSE
CNS Headaches
Mechanism of Paracetamol Overdose:
Tinnitus
Dizziness • Oxidation to a cytotoxic intermediate
CVS Hypertension called N-acetyl-p-benzoquinone mine
Edema (NAPQI) by phase I cytochrome P450
Heart failure enzymes (CYP2E1).
GIT Abdominal pain
Dysplasia • Occurs if substrates for phase II
Nausea conjugation reactions (acetate and
Vomiting glucuronide) are lacking.
Ulcers
Bleeding • Centrilobular region (zone III) - is
HEMATOLOGIC Thrombocytopenia preferentially involved because it is the
Neutropenia area of greatest concentration of
Aplastic anemia CYP2E1.
HEPATIC Abnormal liver
• Antidote is N-acetylcysteine (NAC), a
Function tests
Liver failure sulfhydryl donor.
PULMONARY Asthma DOSAGE of PARACETAMOL OVERDOSE
RASHES All types
Pruritus ✓ Toxic dose: 150mg/kg (21 Paracetamol
RENAL Renal insufficiency 500 mg tabs)
Renal failure ✓ Lethal dose: 15g (30 Paracetamol 500
Hyperkalemia mg tabs)
Proteinuria
TREATMENT of PARACETAMOL OVERDOSE

ASPIRIN: DOSAGE RANGES ✓ Antidote is N-acetylcysteine.

✓ Supportive management
• Low range (<300 mg/d)
 ✓ Gastric decontamination with activated
charcoal.

NSAIDS

Note:

• Ketorolac – NSAIDs (non-selective)

intravenous.

 An effective replacement for

morphine in post-surgical
patient reducing opioid
Note:
requirement by 25-50%.
• Aspirin – anti platelet drug.
 Irreversible.  It has no anti – inflammatory
• Ibuprofen, Mefenamic Acid, effect.
Ketoprofen, Piroxicam – NSAIDs (non-
selective)
 Reversible.
 Preg cat c.
Note: Note:

• Indomethacin – NSAID (non-selective) • Paracetamol – Analgesic.

 Reversible

• Celecoxib – COX2 selective inhibitor.

GLUCOCORTICOIDS FOR NON-ENDOCRINE
• Meloxicam – preferential COX2 selective
DISORDERS
inhibitor.
• A large number of glucocorticoid
preparations - are available for oral,
parenteral, inhalational, or topical
administration for the treatment of a
wide range of inflammatory, allergic,
autoimmune, and other disorders

• Topical administration - is widely used

in the treatment of allergic or
inflammatory conditions affecting the
skin, mucous membranes, or eyes

• Topical ocular glucocorticoids - are used

to treat acute uveitis (inflammation of
the iris, ciliary body, or choroid).
 • Glucocorticoids - are given by inhalation ▪ counteract inflammation
to treat allergic rhinitis, aspiration evoked by physical trauma,
pneumonia, asthma, and other extreme temperatures, noxious
respiratory conditions. chemicals, radiation damage,
and microbial pathogens.
MEDIUM POTENCY, INTERMEDIATE-ACTING
GLUCOCORTICOIDS Examples of diseases treated with
corticosteroids include:
GLUCOCORTICOIDS USES
Prednisone 1. Systemic Lupus Erythematosus
Prednisolone Systemic treatment 2. Autoimmune Thrombocytopenia Purpura
Methylprednisolone 3. Polyarteritis Nodosa
Triamcinolone 4. Multiple Sclerosis
Cancer 5. Ulcerative Colitis
Intermediate-acting Inflammation 6. Polymyositis.
glucocorticoids Allergy
Autoimmune disorders
• Beclomethasone and Mometasone - are
(Duration of action
of 12 to 36 hours) available for nasal insufflation or oral
inhalation to treat allergic rhinitis or
asthma.

HIGH POTENCY, LONG-ACTING

GLUCOCORTICOIDS
• Betamethasone - is available for
systemic use, and it is also used in the
topical treatment of a number of skin
disorders.
▪ Psoriasis
▪ Seborrheic or atopic dermatitis
▪ And neurodermatitis
• Ciclesonide - is a newer agent also
indicated for hay fever or allergic
rhinitis.
• For corneal inflammation and keratitis,
many glucocorticoids - are available in
eyedrops, including a new combination
of loteprednol and the antibiotic
tobramycin.

• Budesonide - is a long-acting • Because of their lymphotoxin effects,

glucocorticoid administered by glucocorticoids - are used in the
inhalation. treatment of lymphocytic leukemias and
lymphomas.
• Budesonide - is also approved for the
treatment of ulcerative colitis. • Betamethasone - is used to prevent
GLUCOCORTICOIDS FOR NON-ENDOCRINE respiratory distress syndrome in
DISORDERS premature infants.

• Glucocorticoids - are frequently used to • Corticosteroids - are often used to treat

suppress inflammation and immune a wide range of dermatologic conditions,
dysfunction associated with diseases including:
affecting almost every organ in the body.
1. Atopic (contact)
 2. Seborrheic dermatitis
3. Pruritus (itching) from various
causes, psoriasis, sunburn, and a
number of other conditions
• Low-potency drugs - are preferred for
treating areas with THINNER skin and
intertriginous areas where skin is folded
or overlapped.
Examples: the face, eyes
• Low- to medium-potency steroids - can
be used on the ears, trunk, arms, legs,
and scalp.
• Medium to very-high-potency drugs -
may be needed to treat disorders in
areas of THICKER skin
Examples: the palms and soles.
• Low-potency topical steroids - include
hydrocortisone.
• Hydrocortisone - is available without
prescription for treating minor allergic
reactions.
• Other low-potency topical steroids
include: desonide and dexamethasone.
• Medium-potency topical steroids -
include triamcinolone and fluticasone.
• Desoximetasone and fluocinonide - are
high-potency steroids, whereas
betamethasone dipropionate and
clobetasol are very-high-potency
steroids
• Glucocorticoids - are used to treat
hypercalcemia, and they are the drugs of
choice for managing sarcoidosis (a
systemic granulomatous disorder).
• Glucocorticoids - are also used as
immunosuppressant drugs to prevent
organ graft rejection.
SYSTEMIC ADMINISTRATION AND
PHARMACOKINETICS
• For acute disorders, glucocorticoids are
often more effective when they are
initially given in large doses that are
gradually tapered over several days until
treatment is discontinued.
• For severe autoimmune and
inflammatory disorders:
Examples:
1. Systemic lupus erythematous
2. Polymyositis with
dermatomyositis
- large doses of prednisone must be
GIVEN DAILY for several months until a
remission is achieved, and then the dose
is slowly tapered and continued for 1 to
2 years or longer.
• In some conditions, it may be possible to
convert the patient to alternate-day
therapy
• This dosage schedule appears to reduce
the severity of adverse effects and
produces less suppression of the
hypothalamic-pituitary-adrenal axis by
allowing more time for recovery
between doses.
• Glucocorticoids - are administered
parenterally to treat acute adrenal
crises, acute allergic reactions, and
similar emergencies.
• In some cases, the drugs are given
intravenously.

• In other cases, they are given

intramuscularly, either as a rapidly
absorbed solution or as a slowly
absorbed drug suspension (depot
preparation).