PHARM250 the Immune system Cheat Sheet by kjaniskevich

Acetam­inophen

Mechanism of action: acts at hypoth­alamus to cause peripheral vasodi­lation, which enables sweating and allows body to rid excess heat
No anti-i­nfl­amm­atory action
Primary use: fever, mild to moderate pain, osteoa­rth­ritis

NSAID

nausea, dyspepsia, ulcer with long-term use, potential anti-p­latelet action, hypert­ension, increased risk of cardiac event with long-term use
Take with food
Caution in kidney disease, cardio­vas­cular disease, GI conditions

Acetom­inophen

very rare liver toxicity (max dose of 4g/24h­ours), avoid alcohol, interacts with warfarin
(but doesn’t ↑ bleeding on its own)

2nd-Ge­ner­ation Antihi­sta­mines

Decongestants
Phenyl­eph­rine, pseudo­eph­edrine

oral – hypert­ension, anxiety, insomnia;
intranasal – nasal irrita­tion, rebound conges­tion, rarely systemic effects

Cephal­osp­orins
Cefotaxime (3rd Gen.)

hypers­ens­iti­vity, rash, itching, anaphy­laxis, diarrhea, vomiting, nausea, pain at injection site, some (minor) drug interactions
Must be given IV or IM (not orally)

Macrolides
Erythr­omycin

: signif­icant nausea, vomiting, diarrhea (take with food), some important drug intera­ctions
Warfarin, cyclos­porine, antico­nvu­lsants (all via CYP450 inhibition/induction)
Fidaxo­micin – new; for treatment of c. difficile; not absorbed, stays in GI tract nausea, consti­pation, vomiting

Fluoro­qui­nolones
Ciprof­loxacin

nausea, diarrhea (can take with food), photos­ens­itivity
Separate from minerals like calcium, iron, magnesium, aluminum (including supple­ments and antacids) by 2h
Serious adverse effects associated with fluoro­qui­nol­ones: Tendinitis or tendon rupture (1.3-5.6 in 10,000)
Cardiac arrhyt­hmias (15-57 in 100,000)
CNS effects  seizures, tremors, altered mental state
Peripheral neuropathy

Carbap­enems
ertapenem, imipenem, meropenem

skin reactions, inflam­mation at injection site, diarrhea, nausea, vomiting

Nitrof­ura­ntoin

Changes urine to orange colour
Must take with food

Vancomycin

Ototox­icity and nephro­tox­icity

Rifampin (RMP)

Rashes, blood dyscra­sias, GI distur­bances, liver damage, nephro­tox­icity
Secretions coloured a reddis­h-o­range (sweat, urine, sputum, tears)

Azole Antifungals
flucon­azole, itraco­nazole, ketoco­nazole, micona­zole, vorico­nazole

Rare hepato­tox­icity – avoid alcohol, watch for jaundice, monitor liver enzymes

Classic Immuno­-su­ppr­essant

Increased risk of infect­ions, Increased risk of cancers such as lymphomas, cysts, and polyps
Frequency increases with intensity and duration of treatment, Kidney impair­ment, hepatic impair­ment, Hypert­ension, hyperlipidemia,
CNS: tremor, headache, skin prickling sensation,
GI: nausea, vomiting, abdominal pain, diarrhea, gingival hyperplasia,
MSK: Muscle cramps, myalgia
Endocrine: Menstrual distur­bances, gyneco­mastia, Hypert­ric­hosis (abnormal amount of hair growth over body), Fatigue

Non-st­eroidal anti-i­nfl­amm­atories
NSAID

Inhibit cyclo-­oxy­genase (COX), which reduces prosta­glandin synthesis therefore inhibiting inflam­mation
Also have analgesic and antipy­retic properties
For mild to moderate inflam­mation

COX-2

more specific for inflam­mation

Mimic endogenous cortisol, attempting to bring body back to homeos­tasis after a fight-­or-­flight response
Anti-i­nfl­amm­atory and immuno-suppressive
For severe inflammation
Serious systemic adverse effects limit use to emerge­ncies and severe inflam­mation (multiple sclerosis, rheumatoid arthritis, auto-i­mmune diseases)
Local admini­str­ation, short-term use preferred whenever possible

Penici­llins
-cillin

Disrupt bacterial cell walls, Bactericidal
Penici­lli­n-b­inding protein: a protein only in bacterial cell walls that penicillin binds to which weakens the cell wall, allows fluid to enter and destroys the cell
Penici­llins contain a beta-l­actam ring in its structure necessary for activity
Many bacteria produce beta-l­act­amase (penic­ill­inase) that is a natural defense to penicillin – it breaks the beta-l­actam ring, leaving it ineffe­ctive therefore penicillin resistance

Drug of choice against strept­ococci, pneumo­cocci, staphy­loc­occi, gonorrhea and syphilis (given IV or IM)

Has broad-­spe­ctrum activity against gram-n­egative organisms; for serious infections of lower respir­atory tract, CNS, genito­urinary system, bones, blood, and joints

Used for Rocky Mountain spotted fever, h.pylori infect­ions, acne vulgaris, chlamydia

Used for upper and lower respir­atory tract infect­ions, whooping cough, diphth­eria, or for other infections in patients who cannot take penici­llins

Used for serious (life-­thr­eat­ening) infections or when other antibi­otics have failed (also topically as eye drops and creams­/oi­ntments – this would not require therap­eutic drug monito­ring)

Used commonly for respir­atory, urinary, ophtha­lmic, gastro­int­est­inal, and gyneco­logical infections – high usage in commun­ity­/ou­t-p­atient

Both drugs inhibit essential folic acid synthesis; work synerg­ist­ically (a pharma­cod­ynamic interaction)
Used to treat urinary tract infections

inhibits protein, RNA, DNA, and cell wall synthesis; bacter­icidal
Excreted unchanged through the kidney (no metabo­lism), therefore used only for urinary tract infections
Changes urine to orange colour
Must take with food

inhibits cell wall synthesis; bacter­icidal (through different mechanism than aminoglycosides)
Reserved for severe infections that are resistant to anything else  usually only used in hospital (methi­cil­lin­-re­sistant staph. aureus - MRSA)
Injection or oral
If IV given too quickly  Red Man Syndrome (flushing, red face, hypote­nsion)  slow down infusion
Therap­eutic drug monitoring required (like aminog­lyc­osides)

2nd-Ge­ner­ation Antihi­sta­mines
Cetirizine (React­ine®), loratidine (Clari­tin®), deslor­atidine (Aerius®), fexofe­nadine (Allegra®)

Decong­estants
Phenyl­eph­rine, pseudo­eph­edrine

Sympat­hom­imetics – stimulants – cause vasoco­nst­riction and reduction of mucous production
For immediate relief of nasal congestion – oral or intranasal
Short term-use only – rebound congestion if longer than 3-5 days (intra­nasal)

Epinep­hrine

Stimulates both α and β adrenergic receptors {{nl} Via α–rece­ptors: counters the high vascular permea­bility that occurs during anaphy­laxis that leads to loss of intrav­ascular fluid and hypote­nsion
Via β–rece­ptors: causes bronchial smooth muscle relaxation and relieves bronch­ospasm, dyspnea, and wheezing
Also alleviates pruritus, urticaria, and angioedema

Binds to fungal cell membranes, making them leaky, Given IV

oral med for fungal nail infections

Because of antire­tro­viral drugs, HIV patients are able to live sympto­m-free for much longer with very low counts of the retrovirus
Antire­tro­viral drugs block the HIV replic­ation cycle

HSV2: genital ulcera­tions

Mostly controlled by oral therapy of antivirals – taken at first sign of outbreak, continued for short term
These antivirals prevent viral DNA synthesis
Very well tolerated – take with food

Lipactin® - heparin + zinc

can reduce pain, may speed healing
Mechanism does not match pathop­hys­iology

Influenza
Amanta­dine, and neuram­inidase inhibitors (oselt­amivir and zanamivir)

BEST PROTECTION = VACCIN­ATION
Antiviral drugs may decrease severity of symptoms of influenza and may shorten symptom time by a couple days IF taken within first 48 hours
Generally used only in patients at high risk of compli­cations from influenza

Calcin­eurin Inhibitors
Cyclos­porine, tacrol­imus, pimecr­olimus (topical)

“Classic” immuno­-su­ppr­essants used for transp­lants (or topically for psoriasis)
Disrupt T-cell function by binding to calcin­eurin
They are not specific – suppress the ENTIRE immune system  patient is very suscep­tible to any other infection
Extensive monitoring for detailed WBC counts and signs of infection (see slide on monito­ring)

medica­tions produced using biological processes in living organisms such as yeast and bacteria
Have active pharma­ceu­tical ingred­ients that cannot reasonably be synthe­sized by chemical means (too complicated)
Are complex, large molecules derived from living sources and produced through a number of intricate steps
Biologics can be immuno­sup­pre­ssant or immuno­sti­mulant (very specif­ically) or replace a substance that is missing (insulin)

not cytotoxic; effects mediated through hormonal receptors (depri­vation) – for hormon­e-r­esp­onsive cancer (breast, prostate, etc.)

monoclonal antibo­dies, tyrosi­ne-­kinase inhibitors (TKIs); the future of treatment – to target cancer cells only

Rifampin (RMP)

Most potent anti-TB drug available
Good bacter­icidal activity, prevents acquired drug resistance and is very important in preventing relapse
Current doses are based on studies performed in the 1960s, when the lowest effective dose was used because of the high cost of the drug; concerns now that dose is too low -> current trials -> dosing recomm­end­ations may change