Professional Documents
Culture Documents
ANTIINLAMMATORY DRUGS
-Eicosanoids -G-protein binding, involved in
-PG, TXA and LT inflammation, toxins, trauma, IgE
reactions
-PGE1 -protective to the gastric mucosa -Abortificient and
contraindicated for
pregnancy.
-Misoprostol -)) -Rx for NSAIDs ulcers
-Alprostadil -Maintains PDA
-PGE2 -uterine contraction
-Dinoprostone -Cervical ripening
during parturition
-PGF2 -uterine and bronchiolar muscle -abortificient
contraction
-Dino/carbaprost -))
-Latanopost Rx of glaucoma
-PGI2 -Vasodilator and inhibits platelet
aggregation
-Activates cAMP - Ca2+ uptake
- intracellular Ca2+ - platelets
stability
-Epoprostenol -Rx for pulmonary HTN
-TXA2 -opposite of PGI2 function
-Activates PLC - IP3 - free
Ca2+ - platelet aggregation
-LT blockers -Headache, dental
pain GI distress and
rash.
-Zileuton -inhibits lipoxygenase Prophylaxis for Asthma -Increases Liver
(immunosuppression) Function Tests
-Montelukast -All lukast drugs are antagonist -)) -headaches, dental
for LTs and block their receptors. pain, GI distress and
-Antagonists for LTD4 receptors rash
-NSAIDs -inhibitors of cyclooxygenase
pathway (Cox1 and Cox2).
-Aspirin -Irreversible noncompetitive -Post MI: baby aspirin -Hypersensitivity
inhibitor of COX 1&2. triad: asthma, nasal
-Works by acetylating the serine polyps and atrophic
residue on the binding site on rhinitis.
COX. -Increases warfarin
-antipyretic, analgesic, anti- toxicity, uricosurics
inflammatory, and antiplatelet and hypoglycemic
aggregation agents.
-Reyes Syndrome:
Aspirin + viral
infection
-Salicylism: chronic
dosing leading to
tinnitus, vertigo and
decreased hearing.
-Acetaminophen -Inhibits COX in the CNS and -Hepatotoxicity:
NOT in the periphery metabolized by
-Therefore only analgesic and Cp450 into reactive
antipyretic metabolite that
damages the liver.
-Antidote overdose:
Acetylcycteine SH
group that inactivates
metabolite
-Reversible -Side effects:
NSAIDs Dyspepsia and
interstitial nephritis
-Ibuprofen -does not affect warfarin and -#1 over the counter pain
hypoglycemic agents unlike reliever
aspirin
-Naproxen -for gout
-Indomethacin -Closing PDA and gout -Thrombocytopenia,
agranulocytosis
-Sulindac -does not affect the kidney -Pancreatitis
-Ketoro/etodo-lac
-Nebumetone
-Diclofenac -hepatotoxicity
-Tolmentin -does not affect oral hypoglycemic
agents.
-Rheumatoid
Arthritis drugs
DMARDs
-Methotrexate -Inhibits Dihydrofolate reductase -Also anticancer -Bone marrow
-Cytotoxic to lymphocytes suppression, Hair
loss, mucositis,
Worsens Nodules
Hydroxychloroquine -Stabilizes lysosomes and decrease -Also for malaria - Cinchonism: GI
chemotaxis distress and visual
dysfunction.
-Hemolysis in G6PD
deficiency
- Sulfasalazine -ASA inhibits COX2 -ASA: GI distress
-Sulfapyridine: decrease B cell -Sulfapyridine: Rash,
functions hemolysis, SLE like
syndrome
-Corticosteroids **REFER TO ASTHMA
ABOVE
-Gold salts -Decrease lysosomal and -Stomatitis, rash,
macrophages functions bone marrow
depression,
Proteinuria and
nephrotic syndrome
-D-Penicillamine -Suppresses T-cell and decreases -Also for Wilsonss -Aplastic anemia,
Rheumatoid factor disease myasthenia gravis
-Suppresses copper metabolites in
Wilsons disease
-Cyclophosphamide -Alkylating agents used in severe -anticancer -Hemorrhagic cystitis
cases
-Azathioprine -Metabolized to 6-Mecaptopurine -Bone marrow
-Inhibits purine synthesis therefore suppression,
immunosuppressive. Leukopenia,
thrombocytopenia,
-hepatotoxicity
-New FDA
DMARDs
1. Infliximab -Monoclonal antibody, Decrease -Infusion reactions,
(Remicaids) TNF infections
2. Etanercept (Enbrel) -A recombinant of TNF receptor -Also for treating -Hypersensitivity,
that Binds to TNF Psoriasis infections
3. Leflunomide -Pyrimidine synthesis inhibitor -Alopecia, rash,
-Inhibits dihydro-orotic acid hepatotoxicity.
dehydrogenase decreased UMP
decreased RNA.
4. Anakinra -IL-1 receptor antagonist -Reaction at injection
site, infection
5. Adalimumab -Recombinant Monoclonal
(Humira). antibodies
Binds to TNF
-Osteoarthritis drugs -Tylenol and Celecoxib **REFER TO NSAID AND COX
2
-Osteomyelitis -Ox/Clox/Diclox and -For Staph Aureus
drugs Naf
-Fibromyalgia drugs -Cymbalta (duloxetine) -SNRIs antidepressant -Also for chronic pain
and DM neuropathy.
-Pregabalin (Lyrica)
-Polymyalgia -Steroids -Give 15mg initially, taper off. If -usually present with
Rheumatica drugs symptom persists, give 40mg, if temporal (giant cell)
not they go blind. arteritis.
-Gout (Crystal
induced Arthritis)
NSAIDs -Indomethacin, **REFER NSAID ABOVE -initial treatment
Sulindac, Naproxen
-Colchicine -binds to tubulin decreases -Acute gouty attack -Acute: Diarrhea and
microtubule formation GI pain
-decreases LTB4 -Chronic:
Mylosuppression,
-Inhibits leukocyte and peripheral
granulocyte migration neuropathy,
hematuria and
alopecia
` -Allopurinol -Inhibits Xanthine Oxidase via -Chronic gouty arthritis -Peripheral
suicide inhibition neuropathy, stone
-*inhibits 6-mecarptopurine formation, rash,
metabolism vasculitis
-Probenicid -Inhibits proximal tubular -)) -urate crystals in the
reabsorption of urate kidney
-inhibits secretion of acidic drugs:
Penicillins
-Sulfinpyrazone -similar to Probenicid. -GI distress, rash,
-Activity is GFR dependent (not nephrotic syndrome
good below 30ml/min)
-Inhibits platelet aggregation
DRUGS IN IMMUNOLOGY
-For organ
transplant
1. Cyclosporine -Binds to cyclophillin leads to - Nephrotoxicity,
decrease calcineurin - inhibition Gingival Hyperplasia
of transcription factors IL-2, IL-
3 and INF
-usually administered with
corticosteroids
2. Azathioprine -*REFER TO DMARDS
3. Muromonab-CD3 -Monoclonal antibody -Acute renal transplant
-Must administer rejection
methylprednisone before IV
Muromonab-CD3 (to counteract
initial flaring and prevent cytokine
release syndrome)
4. Sirolimus -it inhibits signal transduction -Nephrotoxicity
(Rapamycin) -Sirolimus is metabolized by
cytochrome P450
5. Tacrolimus (FK506) -calcineurin inhibitors -renal and liver
transplants
6. Mycophenolate -inhibits de novo synthesis of
Mofetil (MMF) purine by inhibiting IMP
dehydrogenase
-Used in combination with
cyclosporine
-Rh Incompatibility RhoGAM -Administer at 28wks of
pregnancy and 72 hrs after
parturition if the baby is positive
ONLY if the mother didnt
develop antibodies and therefore
still negative
-If mum Rh is positive, then titer
measure
-Cytokines in
Clinical Use
-INF -Hepatitis, leukemia
-INF -MS
-INF -Chronic Granulomatous
Disease
-IL-11 -Thrombocytopenia
-Thrombopoietin -Thrombocytopenia
-Erythropoietin -Anemia
- Aldesleukin (IL-2) - Renal cell Carcinoma
- Filgrastim (G-CSF) -bone marrow recovery
- Sargramostim (GM- - bone marrow recovery
CSF)
Monoclonal
Antibodies in
Clinical Use
- Abciximab - IIb/IIIa receptors inhibitor - antiplatelet indicated
after PCI (stent)
-Infliximab -Rheumatoid arthritis
-Omalizumab -Asthma
-Trastuzumab -Breast Cancer
-Daclizumab -Renal transplants
-Muromonab -Renal transplants
-Palivizumab -RSV(repiratory
syncytial virus)
-Rituximab -Non-Hodgkin
Lymphoma, lymphoma
-Adalimumab -Rheumatoid arthritis
Antibiotics
1. Inhibition of cell -Penicillins -Bind to cytoplasmic-penicillin- -Penicillin: gram ve,
wall synthesis Cephalosporins binding proteins (PBPs) Neisseria, syphilis,
Imipenem, meropenem, Inhibit transpeptidation Rheumatic fever
aztreonam inhibit cross-linking of bacterial
cell wall
-Bactericidal
C. Interfere with the -Chloramphenicol -Bacteriostatic How?: Inhibition -Gray baby syndrome
formation of of peptidyltransferase
peptide bond
5. So they came up -Clavulanate and -inhibit B-lactamase inhibitors - and combined it with
with B-lactamase sulbuctam, Tazobuctam broad spectrum and
inhibitors extended spectrum to
cover everything
including staph aureus
-Inhibitors of the -Tetracycline (both Tetracycline - -Used in patients allergic to -Good for chlamydia, 1. Contraindicated in
A site generic and brand Doxycycline- penicillin Rickettsia, Mycoplasma, children younger than
name) Minocycline- -Dairy product should be avoided Brucella, Yersinia and 8y/old why?
Demeclocycline with Tetracycline why? reduce Vibrio cholera, lyme permanent
absorption (Chelators) Except disease discoloration of
doxycycline & Minocycline teeth
3. Out dated
Tetracycline:
Fanconi like
syndrome
4. Hepatotoxicity:
more in pregnant
women
-Tetracycline
-Demeclocycline -inhibits ADH -and used to Rx SIADH 5. Nephrogenic
seen in small cell lung diabetes insipidus
cancer.
-Doxycycline -penetrates the prostate
and used in Prostatitis
-chlamydia
-mostly intracellular
microbes (obligate
intracellular)
-Minocycline 6. Vestibular
Ototoxicity
(Minocycline)
All tetracyclines, except doxycycline (fecal excretion) require dose adjustment in renal impairment
-Inhibitors of DNA -Fluoroquinolones -Ciprofloxacin, -Inhibit DNA gyrase -Drug of choice: -contraindicated for
synthesis Norfloxacin, Ofloxacin (topoisomerase II) Anthrax pregnancy
Enoxacin, Trovafloxacin -2nd choice: Penicillins -Careful <18y/old
or tetracyclines why? inhibit
-Good against Gram-ve chondrocytes
sepsis (PO)
-Sparfloxacin -Resistant
pneumococcus
-Ofloxacin -Chlamydia
-Inhibitors of -Aminoglycosides -Gentamycin - -Active transport by O2 -gram-ve infections 1. Ototoxicity (2%)
Initiation Tobramycin - dependant system Auditory:
Paromomycin Irreversible
Amikacin- Neomycin- -***Cannot be used to treat (cochlear), high pitch
Kanamycin- anaerobic infections 1st
Streptomycin Vestibular:
-All aminoglycosides require Reversible
dose adjustment in renal failure
2. Nephrotoxicity:
(7%)
Proteinuria,
hypokalemia, and
acute tubular necrosis
3. Neuromuscular
blockade
Decrease
prejunctional release
of Acetylcholine
-Amphotericin B, 2. Enhanced
Vancomycin, Cisplatin, Nephrotoxicity
cyclosporin
2. Hemolysis in
G6PD deficiency
3. Photosensitivity
4. Crystalluria
Antituberculous drugs
1. Isoniazid (INH) -MOA: Inhibition of mycolic acid -Hepatitis
synthesis (Cell wall synthesis) -Neuritis
-Hemolysis in G6PD
-Resistance: deficiency
Low resistance: Deletion in INHA -SLE in slow
gene; gene encoding acyl carrier acetylators
protein (Target)
-DMAC: -Azithromycin +
Disseminated Rifabutin + Ethambutol
Mycobacterium
Avium Complex
-Mesoridazine -**Prolonged QT
interval
- Torsade de pointes
-Clozapine -***Agranulocytosis,
weight gain, seizure
-Antidepressants
1. Tricyclic [TCAs] -Inhibit reuptake of NE, serotonin
-SNDRIs and dopamine
-contraindicated in pregnancy
-All triptyline and pramines
are TCAs except for Doxepin
-Amitriptyline -used for chronic pain
-Nortriptyline (DM pains and shingles
zoster pain, or pain
without etiology)
-Maprotiline -seizures
-Mirtazapine -Potent anxiolytic drug (behave) -Anxiety, anorexia and -seizures and
insomnia agranulocytosis
-Phenelzine,
isocarbazide,
selegiline(MOA-B)
-Tranylcypromine
6. RIMA -Moclobemide -Reversible Inhibitors of MAO-
Broforamine A
7. SSRI -Selective Serotonin Reuptake -GI symptoms (rare)
Inhibitors -Sexual dysfunction
-All SSRI are safe in Pregnancy, -Insomnia
less side effects
-Sertraline (Zoloft)
-Antianxiety Drugs -Panic Disorder -Alprazolam -Drug of Choice -For acute panic attack
-Hydroxyzine -Antihistamines
Toxicology
-Heavy Metal -Type -Antidote -Clinical Presentation/ MOA -Etiology -Other
1. Lead Poisoining -Acute: GI distress (lead colic), -Pica during pregnancy
tinnitus, encephalopathy lead poisoning in the
-Chronic: anemia (decrease new born mental
heme), wrist drop (affected radial retardation
nerve), proteinuria, decrease
fertility
Anticancer Drugs
2 types of drugs against cancer:
1. Cell-cycle specific (acts on cell undergoing division)
In general, CCS drugs are most effective in high growth fraction tumors
2. Cell-cycle nonspecific (acts on cell during any phase)
useful in low growth fraction solid tumors as well as in high growth fraction tumors
One of the reason for use of drug combination is because of the log-cell kill hypothesis (kills in logs of 3)
-Cell Cycle
1. Non phase -Alkylating agents
specific (CCNS) -Nitrosourea
-Decarbazine
-Cisplatin
-Antitumor
antibiotics
2. Phase Specific
(CCS)
-Dacarbazine (MM)
-Altretamine (OC)
2. Antimetabolites
B. Pyrimidine -5- FluoroUracil (5FU) - Fluoro -deoxyUridine- -Cancer cells -nausea, mucositis,
Antagonist MonoPhosphate (FdUMP) diarrhea, hand and
-Inhibits thymidylate synthase foot syndrome
thymineless death
-FUTP (Triphos.): interferes
with RNA processing
-Flucytosine -Fungal cells
B. Taxanes 1. Paclitaxel (Taxol) -enhancement of tubulin -breast, lung and ovarian -Alopecia, arthralgia,
polymerization cancer peripheral
-Prevents the separation of tubulin neuropathy
dimers.
-metabolized by cytochrome P450
-Tyrosine kinase
inhibitors
-Imatinib (GLEEVEC) -inhibitor of tyrosine kinase -first line therapy in
domain Bcr-Abl oncoprotein chronic phase of CML,
-prevents the phosphorylation of and blast crisis
kinase substrate by ATP -GIST
-Growth factor
receptor inhibitors
-Gefitinib (IRESSA) & -small molecule inhibitors of the -used in non-small cell
Erlotinib (TARCEVA) tyrosine kinase domain lung cancer
associated with the EGFR
(Epidermal Growth Factor
Receptor )
Resistance to Chemotherapy
1. Formation of cancer drug inactivating enzymes (alkaline phosphatase for 6MP): 6-Mercaptopurine and 5-Fluorouracil
2. Decrease of binding affinity and drug sensitivity: Etoposide, methotrexate, vincristine, vinblastine
3. Decrease drug accumulation or permeability (by expulsion): Methotrexate, dactinomycin, cyclophosphamide
4. Chemical reactions inactivating chemotherapy (conjugated by glutathione and excreted in feces): Cyclophosphamide, bleomycin, cisplatin
5. Increased nucleic acid repair mechanism: Cisplatin, Cyclophosphamide
6. Reduced activation of pro-drugs: 6-Mercaptopurine, 5-Fluorouracil
7. ***Multidrug resistance:
increased expression of MDR1 gene for P-glycoprotein
overexpression of the multidrug resistance protein 1 (MRP1)
Antifungal
Opportunistic infections: cryptococcosis and aspergillosis
Hospital-associated infections: candidemia
Community-acquired infections: coccidioidomycosis (valley fever), blastomycosis, and histoplasmosis
A. Polyene 1. Amphotericin B -MOA: Binds to ergosterol -IV for serious and life -Dose dependant
Antifungal (Fungicidal) threatening infections -Nephrotoxic
-Gets inserted to membranes and -Severe fungal -Hypokalemia: renal
forms micropores pneumonia, tubular acidosis,
-cryptococcal severe Mg+ and K+
-For the flu-like symptoms: meningitis wasting
Premedicate patients with -Disseminated -Normochromic
antipyretic, antihistaminic and infections normocytic anemia
antiemetic agents histoplasmosis,
coccidiodomycosis -Infusion dependant
-Distribution: Low penetration reactions (cause
into CSF No BBB crossing -Aspergillus fumigatus, release of
(Given intrathecally) -Candida albicans, prostaglandins)
-Cryptococcus -Flu-like symptoms
-Drug Interactions: synergistic Neoformans, -fever, nausea and
with fluocytosine -Histoplasma vomiting
capsulatum
-Resistance: Decreased ergosterol -Blastomyces
levels and decreased affinity dermatitidis
-Coccidioides immitis
-Fluconazole is often given after -Mucor
an aggressive treatment with
amphotericin B -Rx of resistant
Cryptococcus and
-Not absorbed in the GI thus given candidiasis
intravenously.
-Resistance: Decrease
intracellular levels of drugs due to
decreased entrance of the drugs
into the cell
-Clotrimazole and -given topically -Rx of candida and
Miconazole dermatophytic infections
-Antifungal with 1. Griseofulvin -MOA: Disruption of mitotic -Rx of tinea cruris - Increase effects of
limited indications spindle by interfering with (Jock itch) alcohol (disulfaram-
microtubules like action)
-Contraindicated in
-Given orally and for a long time intermittent porphyria
because it is fungistatic -Induces Cyt P450
-esophageal candidiasis
and invasive
candidiasis
AntiViral
-Avir: for AIDS
-Ivir: for influenza
-Anticholinergic
effects
A. Indinavir -Nephrolithiasis
-Hyperbilirubinemia
-Inhibition of p450
6.CCR5 -Maraviroc
Antagonists
HIV drugs are used in combinations
"Drug cocktails"
HIV cocktail: HAART; Highly Active AntiRetroviral Therapy
Acquired Immune Deficiency Syndrome (AIDS)
Treatment is based on CD4 cell count
What's recommended?
2+1
Any 2 Nucleosides inhibitors + 1 Protease inhibitor
2 of (AZT, DDI, 3TC, D4T) + 1 of (Indinavir or Ritonavir)
3. If CD4 < 75
Mycobacterium Avium Complex (MAC) prophylaxis
Azithromycin, Clarithromycin (MACrolides for MAC)
4. If CD4 < 50
Cytomegalovirus Prophylaxis
Ganciclovir
HIV Transmission
Needle stick: 1:300
Anal receptive: 1:50-100
Vaginal: M to F: 1:1000, F to M: 1:2000-3000
Pregnant mom to baby: 25%
Pregnant taking AZT: 8%
-Aspirin -Irreversibly inhibits COX1 and -Prophylaxis in MI and -Gastric ulcer and
COX2 stroke bleeding
-Antiplatelets (low doses) and
Antiinflammatory
3. Antiplatelets that -IV Abciximab -Prevent platelets aggregation by -Acute coronary disease
inhibits IIb/IIIa -Eptifibatide inhibiting fibrinogen from -Angioplasty
receptors -Tirofiban binding to IIb/IIIa receptors -PCI
-Antidote to Warfarin:
Vit K1 (Phytonadione)
Contraindications
1. Hypersensitivity
2. Underlying coagulation disorder
3. Ulcer disease
4. Severe thrombocytopenia
5. Active bleeding
Adverse reactions
1. Thrombocytopenia [(HIT): 10-14 days after heparin]
2. Pain at site of injection
3. Spinal and epidural hematoma should be avoided in lumbar puncture, regional anesthetic block
-Fibrinolytics
Mechanism of Action of thrombolytics
whaActivate conversion of plasminogen to plasmin
Plasmin cause lysis of fibrin clot to degradation products
Plasmin is a serine protease and is inhibited by alpha2 antiplasmin
Indications:
Acute MI, Acute PE, DVT, superior vena caval syndrome, ascending thrombophlebitis, Acute Ischemic stroke
Has to be used btw 6hrs of acute MI (STEMI and bundle branch block)
-for ischemic stroke, has to be used within 3hrs
Topical hemostatic
Used during surgery to limit blood loss
Absorbable gelatin sponge ( Gelfoam)
Absorbable gelatin powder
Microfibrillar collagen hemostat (MCH)
Thrombin
Antiprotozoal
-Metronidazole 1. Giardiasis: Giardia
Lamblia
Most common water
born disease, Back-
packer's diarrhea
2. Amebiasis:
Entamoeba Histolytica.
3. Trichomoniasis:
Trichomonas vaginalis
Gotta Rx the partner
-Diloxanide, Iodoquinol -Asymptomatic/non-
and Paramomycin invasive intestinal
(luminal) amebiasis
-Nifurtimox 5. Trypanosomiasis:
Trypanosoma cruzi
-American
Trypanosomiasis
(Chagas disease)
-Trimethoprin- 7. Pneumocystosis:
Sulphamethoxazole Pneumocystis carinii
(TMP-SMX or
Cotrimodazole)
-IV Pentamidine
-Atovaquone
-Malaria
-Chloroquine -inhibits the polymerization of 8. Malaria:
heme caused by plasmodium
-Plasmodium
Falciparum (No relapses
or reoccurrence)
-Plasmodium Malariae
Adverse effects of -Chloroquine -Has high volume thus deposits in -First sign: Tinitus
antimalatial drugs organs. Pruritis, ocular
(****Look the dysfunction,
tables in ppt) hemolysis
-Avoid in psoriasis
-Mefloquine -Syncope,
extrasystoles.
-Avoid in seizure and
cardiac arrhythmias
-Primaquine -Neutropenia,
hemolysis
-Avoid in pregnancy,
G6PD deficiency.
-Quinine -Cinchonism, CNS
defects, hemolysis,
black water fever
-Avoid in pregnancy
SAND: Strongyloides,
Ancylostoma, Necator
Cholinergic pharmacology
Muscuranic receptors: M2 found in the heart, M1 GIT glands and M3 everywhere else
Effects of the activation of the receptors:
Eye: Miosis and accommodation
Heart: Bradycardia, decreases HR(SA node) and conduction velocity (AV node) (M2)
Lungs: Bronchospasm and secretion
GIT: Increases motility, secretion (M1), contraction-diarrhea
Bladder: Contraction (detrusor), sphincter relaxation, voiding, urinary incontinency
Sphincters: Relaxation except for the LES (contraction)
Glands: Salivation and secretion and lacrimation
Blood Vessels: Dilation via NO
M1 and M3 via Gq: Increase phospholipase C leading to increase IP3, DAG, Ca++
M2 via Gi: decrease adenylyl cyclase leading to decrease cAMP
Nn and Nm: No 2nd messenger. Activated by opening Na/K channels
-Muscarinic
Agonists (Direct
acting)
- Pancuronium
-Rx: Dantrolene
Adrenergic Pharmacology
Refer to ppt for some information
3. NE metabolism (Termination of action)
a. Uptake through NE transporter system
b. activation of alpha 2 receptors inhibit release of NE
c. MAO metabolizes NE at prejunctional levels.
2 Forms of MAO:
MAO type A: Buzz word: metabolizes NE, 5HT, and tyramine
e.g.: Phenelzine and tranylcypromine (inhibitors) - Rx of depression
MAO type B: Buzz word: metabolizes Dopamine
e.g.: Selegiline (inhibitors)- Rx of Parkinson's disease
d. Catechol-O-Methyl transferase (COMT) metabolizes NE postjunctional at target cells
Buzz word on drugs affecting NE:
1. Interference with Synthesis: methyl-p-tyrosine
2. Displacement of Mobile Pool (indirect acting sympathomimetic): Amphetamine and ephedrine
3. Blockade of Reuptake of NE (indirect acting sympathomimetic): Cocaine and Tricyclic antidepressants
4. MAO inhibitors: inhibit metabolism of NE; Phenelzine, Tranylcypromine and Selegiline
5. Blockade of granular uptake: Reserpine used in Hypertension
6. Blockade of release from granules: Guanethedine used in Hypertension
7. Presynaptic alpha 2 agonists: Clonidine, methyldopa: used in Hypertension
3. Selective B2
agonists
-2. Phenoxybenzamine -Blocks alpha 1, alpha 2 -Short term use (drug of -reflex tachycardia,
-non competitive (irreversible) choice) in miosis, inhibition of
-makes covalent bond with alpha 1 pheochromocytoma ejaculation
receptors
-Selective alpha 1 -Prazocin - Doxazocin -Less reflex tachycardia because -Rx of Hypertension and -Elderly get syncope
blockers Terazocin (not used of NE feedback by alpha 2 is BPH
much anymore) intact
-Propranolol -is the first beta blocker and is non -Increase LDL and
selective TGs
3. CNS depression (cross BBB)
1. Diuretics
-Increase plasma
cholesterol and TGs
(except indapamide)
2. Loop Diuretics -Furosemide -Inhibit the Na+/K+ dichloride -Indicated for -Hyponatremia,
-Bumetanide (2Cl-) cotransport system hyperalcemia (myeloid hypokalemia,
-Torsemide -Increase excretion: Na+, K+, leukemia) hypomagnesia,
-Ethacrynic acid Mg++, Cl, HCO3, Ca++ Metabolic alkalosis,
-Crossallergy to sulfa drugs Hypocalcemia
EXCEPT for Ethacrynic acid -Ototoxicity (EA
-loop diuretic + Antibiotic >furo)
(aminoglycosides): Increased
risk for Ototoxicity
3. Osmotic -Mannitol -Increase the osmotic pressure in -Rx of Increase -Acute hypovolemia
Diuretics -Urea the proximal tubule leading to intracranial and
inhibition of reabsorption of water intraocular pressure
and electrolytes -Acute renal failure
-Oligohydramnios,
IUGR,
hypocalvaria, Renal
failure.
- Captopril -Captopril
- Lisinopril associated with
angioedema
- Enalapril - IV for hypertensive
emergency
- Fosinopril -no dose adjustment in renal
failure
-Atenolol, Pindolol
-Labetalol -Hypertensive
emergency/crisis
(BP>180 and
symptomatic)
-Carvedilol -for compensated heart
failure
5. CCB (Calcium -Drugs ending in ".dipine" -Angina pectoris,
Channel Blockers) except for Diltiazem and peripheral vascular
Verapamil disease,
-block the L-type Ca++ channels tachyarrhythmia.
-African American and elderly
respond well
6. Alpha 2 agonist -Clonidine -patches cause less side effects -Mild to moderate -Edema, rebound
Hypertension hypertension after
sudden withdrawal
-Alpha methyl dopa ****Safe in pregnancy and renal -Mild to moderate -+ve Coombs test:
dysfunction hypertension hemolytic anemia
(due to hapten
formation)
7. Adrenergic -Guanethidine -Binds to storage vesicles and -Fluid retention
Neurononal inhibit release of NE -Contraindicated
Blocking Drugs with
Antidepressants
9. Direct acting -Hydralazine -Relaxes arteriolar smooth muscle -moderate to severe -Reflex tachycardia,
Vasodilators -Safe in Pregnancy hypertension palpitations (use a
BB)
-SLE like syndrome
and hemolytic
anemia
-***Sodium -Dilate both resistance and -Drug of choice for Rx -accumulation of
Nitroprusside capacitance vessels of hypertensive crisis cyanide and
-Administer with nitrites and (IV) thiocyanate
thiosulfate to chelate CN-
-Minoxidil -A prodrug which after sulfation -Rogaine (Topically) for -Hypertrichosis
appears to activate ATP dpt K+ baldness (excessive hair
channels growth)
Antiarrhythmic Drugs
(ppt 2 Slide #1 - #7)
4 Classes
Class 1: Na+ Channels Blockers
Class 2: Beta Blockers
Class 3: K+ Channels Blockers
Class 4: Calcium Channels Blockers
-Class 1 and 3 are the BIG GUNS: for life threatening arrhythmia
Class 1: Na+
Channel Blockers
Class 4: Calcium -Verapamil & Diltiazem - SA & AV nodal conduction and -Rx of PSVT due to AV -Contraindicated in
channel Blockers slope of phase 4 nodal re-entry atrial tachycardia due
to WPW (tissue
problem)
Torsades de pointes
Management
Discontinue the drug prolonging the QT
K+ channel blockers, thioridazine, TCAs
Correct hypokalemia & Hypomagnesemia
Magnesium is indicated
Myocardial Infarction
Goal of Treatment
Relieve chest pain, Stabilize the heart rhythm, Reduce cardiac workload
ER Management of Myocardial Infarction
1. Oxygen
2. Morphine for pain and anxiety
3. Nitroglycerin sublingually
4. Aspirin to chew on (prevents platelets aggregation)
5. Beta blockers to decrease cardiac rhythm
6. ACE inhibitors to reduce preload and afterload
7. Buzz word: Thrombolytics to dissolve blood clots
Heart Failure
Goal of treatment of Heart failure
1. Drugs that increase contractility
2. Drugs that decrease preload
3. Drugs that decrease afterload
4. Drugs that reduce edema
Antihyperlipidemic Drugs
Cholesterol lowering drugs
(PPT #4 16-17)
1. Statin -Atorvastatin -(drugs ending in "Statin") -Hyperlipoproteinemia -Myopathy: From
Simvastatin, Pravastatin -(HMG-CoA reductase -Hypercholesterolemia muscle ache,
Inhibitors) -Hypertriglyceridemia myalgia, myositis to
-(3-Hydroxy-3-MethylGlutaryl Statin are used for 2ry rhabdomyolysis
CoA reductase inhibitors) prevention of heart (break down of
-Statin inhibit the rate limiting disease skeletal muscle)
step in cholesterol biosynthesis renal failure
-Statin reduce LDL, cholesterol,
and triglycerides
-Statin increase HDL (Good
Cholesterol)
-Statin increase NO and decrease
mRNA for endothelin-1
vasodilation
2. Bile acid -Cholestyramine -Bind bile acids in the GI form -Special indication for -Not used in
Sequestrants Cholestipol an insoluble complex that is Cholestyramine : Rx of hypertriglyceridemia
excreted in the feces. So pruritis due to biliary because they increase
cholesterol is used to make more obstruction. How? In VLDL and TG
bile acid thus lowering LDL (bad biliary obstruction the -Constipation
cholesterol) liver can't eliminate bile -Malabsorption of Fat
soluble vitamins
(ADEK)
-Malabsorption of
digoxin, thiazide, and
warfarin
4.Antacids: -Na HCO3 (Alka- -Neutralize gastic acid -intermittent heartburn - Drug interactions
Selzter), Al(OH)3 , -Raise the antral pH > 4 and dyspepsia (form complexes with
Mg(OH)2 , Ca CO3 -may also promote mucosal -GERD tetracyclines and
(Tums) defense mechanisms fluoroquinolones
and makes them
unabsorpable)
***H-Pylori Triple therapy: Drugs: amoxicillin, clarithromycin, tetracycline and metronidazole + PPIs (2 antibiotics +1PPI): triple therapy
(metronidazole if allergic to penicillin)
Antiemetics -Anticholinergics -Hyoscine - MOA: block cholinergic -Rx of motion sickness -high incidence of
(Scopalamine) pathway - vestibular apparatus (kinetosis) anticholinergic
-Dicyclomine effects
-H1 -Promethazine -Motion sickness, chemo -highly sedative
Antihistaminics (Phenargan) induced vomiting
-Diphenhydramine
(Benadryl)
-Cyclizine
-Cinnarazine
Drugs used to treat -Aminosalicylates - 5-ASA bound by an azo (N=N) -Ulcerative colitis and
Inflammatory bond to an inert compound or to Crohn's disease
Bowel Disease another 5-ASA molecule
(IBD) - 5-ASA drugs induce and
maintain remission in ulcerative
colitis
-first-line agents for treatment of
mild to moderate active ulcerative
colitis.
-Crohn's disease - first-line
therapy for mild to moderate
disease involving the colon or
distal ileum.
-Sulfasalazine - 5-ASA + Sulfapyridine
[trasporter to deliver ASA to the
colon, to prevent destruction in the
upper GIT]
-olsalazine
-balsalazide
Bile acid therapy for -Ursodiol -Ursodiol decreases the cholesterol - Ursodiol is used for
gallstones content of bile by reducing hepatic dissolution of small
cholesterol secretion cholesterol gallstones in
patients with
symptomatic gallbladder
disease who refuse
cholecystectomy or who
are poor surgical
candidates