PHARMACOLOGY Flashcards
A centrally-acting antihypertensive that is associated with lupus like syndrome
Methyldopa
Adrenoreceptors that causes mydriasis, ejaculation and vasoconstriction of peripheral circulation
Alpha 1
Selective beta blocker that has a very short half-life and is used to treat intraoperative hypertension.
Esmolol
Calcium channel blocker utilized to treat vasospasm in Subarachnoid hemorrhage due to a ruptured cerebral aneurysm
Nimodipine
A non-dihydropyridine calcium channel blocker that causes constipation and is contraindicated in heart failure
Verapamil
autonomic or somatic system? Associated with skeletal system
somatic
autonomic or somatic system? regulation of very important organs such as lungs and heart
Autonomic
Sympathetic
Thoracolumbar division
Parasympathetic
Craniosacral division
Predominant neurotransmitter in sympathetic preganlionic
ACH
Predominant neurotransmitter Sympathetic preganglionic
ACH
Predominant neurotransmitter Parasympathetic postganlionic
ACH
Predominant neurotransmitter Sympathetic postganglionic
NE
cholinergic receptor that supplies the sweat glands and some specialized blood vessels
Muscarinic
Cholinergic receptor indirectly stimulated by malathion or organophosphate
Muscarinic
Adrenergic receptor involved in peripheral vasoconstriction
Alpha 1
Adrenergic receptor abundant in heart
Beta 1
Adrenergic receptor abundant in lungs
Beta 2
Alpha 1 receptor agonist for treatment of septic shock
Norepinephrine (Levophed)
Alpha 1 blocker which is used to treat BPH
Prazosin
Terazosin
Tamsulosin
Side effect of alpha 1 blockers for treatment of hypertension
Orthostatic hypotension/ 1st dose hypotension
Side effect of beta blockers (beta 2)
Bronchoconstriction
Bradycardia
Beta 2 agonist tocolytic
Terbutaline - used for asthma
Ritodrine
Isoxuprine (duvadilan)
Alpha 1 selective agent used for nasal decongestion
Phenylephrine
Oxymethazoline
Side effect of phenylephrine
Hypertension
Rebound hyperemic or nasal congestion. Occurs in 3 days of use of nasal sprays
Rhinitis medicamentosa
Alpha 2 selective agonists useful for management of hypertension which causes lupus like syndrome and can be used in pregnancy
Methyldopa
DOC of Pre eclampsia
Methyldopa
Beta 1 selective agonist used for management of cardiogenic shock (hypotension) on acute heart failure
Dobutamine
Beta 2 selective agonist used for asthma as relievers
Terbutaline
Salbutamol
Fenoterol
Cholinergic antagonist given to COPD patients in combination to beta 2 agonist (like salbutamol or fenoterol)
Ipratropium
Side effect of Beta 2 agonist
Hypokalemia
Muscle tremors (Terbutaline)
Tolerance
Tachycardia
causes depression or suicide tendencies
Reserpine
DOC for treatment of pheochromocytoma
Phenoxybenzamine
Adrenal medulla tumor
Pheochromocytoma
Parasympathetic agents - Cholinergic agonist
DDUMBELS
Diarrhea
Decrease BP
Urination
Miosis
Bronchoconstriction
Excitation of skeletal muscle
Lacrimation
Salivation and sweating
= Organophosphate poisoning
Direct acting cholinomimetic DOC for Post op urinary retention
Bethanichol
Direct acting cholinergic agonist used as eyedrops
Pilocarpine
DOC for Myasthenia Gravis
Pyridostigmine
Physostigmine
Neostigmine
DOC for glaucoma
Carbachol
Pilocarpine
Cholinergic antagonist associated with malignant hyperthermia
Succinylcholine
or halothane
DOC for malignant hyperthermia
Dantrolene
Antimuscarinic acts as anti-motion sickness
Anterograde amnesia
Scopolamine
Morphine + scopolamine “twilight sleep”’
Famous anticonvulsant that binds to synaptic vesicle protein (SV2)
Metabolized int he kidney
Leviteracetam
Actions of the body on the drug
PharmacoKinetics
Katawan
Major organ where the drug metabolized
Liver and kidney
Actions of the Drug on the bidy
PharmacoDynamics
Drug has affinity for receptros but no ability to activate them
Antagonist
Dose required to cause one half of individuals
ED50 / Median dose
LD 50 divided by ED50
Therapeutic index
RATE and EXTENT of drug absorption from a dosage form
Bioavailability
Transfer of drug from of administration to bloodstream/systemic circulation
SITE of admin TO BLOOD
Drug absorption
Absorbable or Excretable drug?
NON-POLAR
LIPID soluble
NON IONIZED
Absorbable
Study of RATE PROCESSES involved in absorption, distribution, metab and excretion of drug
What the BODY DOES TO DRUG
PharmacoKinetics
Basic pharmacokinetic processes (ADME)
Absorption
Distribution
Metabolism
Excretion
Drug DISPOSITION (DME)
Distribution
Metabolism
Excretion
Drug ELIMINATION (ME)
Metabolism
Excretion
Relationship between drug concentration at the site of action and pharmacologic response
Drug DOES TO THE BODY
“Mechanism of action of drug”
PharmacoDynamics
A drug with both affinity and intrinsic activity
Agonist
A drug with affinity but NO intrinsic activity
Antagonist
Drug disposition commences with which of the pharmacokinetic processes
Distribution
Drug elimination commences with which of the followinh pharmacokinetic processes
Metabolism
Refers to the amount of drug in the blood stream
Greatly affected by drug absorption
Bioavailability
Route of administration with NO absorption, 100% bioavailability and no loss of drug
IV (intravenous)
“Depot effect” (storage effect) can be achieved
IntraMuscular (IM)
Basis why acidic drug is best absorbed in the stomach
Henderson-hasselbach equation
Most important site of drug absorption
Small intestine (DUODENUM - BEST!!)
*except for acidic drugs!!
Site of absorption for SLOWLY absorbed drugs
Large intestine
Rate at which the drug solution leaves the stomach and enters the duodenum
Gastric emptying rate
The ony drug that has higher bioavailability when ingested with fatty meal!
Griseofulvin
Normally, fatty meal (as well as high carb meal) DECREASES drug bioavailability.
HOT foods Increases GER
INCREASE o DECREASE?
Lying on the LEFT side?
DECREASE GER
INCREASE o DECREASE?
Lying down vs Standing?
DECREASE GER when LYING DOWN
Antiemetics like metoclopramide will __(increase or decrease)__ GER?
Increase
Is there First pass effect in Middle rectal vein and Inferior rectal vein?
NO. It will no go to the hepatic portal system (Superior Rectal Vein only)
Reversible transfer of drug from one compartment to another
Distribution
Most important contributory factor that affects drug distribution
Perfusion (q)
Basis of computation of the loading dose
Volume of distribution of a drug
Conversion of a drug to an excretable form
Metabolism
Phase 1 reactions (RedOx reaction) :
HORD
Hydrolysis
Oxidation
Reduction
Deamination
Most important site of drug metabolism
Liver!
Kidneys, intestines, skin, heart
Danger of enzyme inducers
Low therapeutic effect
Danger of enzyme inhibition
Toxicity
Enzyme inducers:
Phenobarbital
Phenytoin
Rifampicin
Carbamazepine —AUTOINDUCTION
Barbequed/ charboiled/ cigarette smoking
Chronic alcoholism
St johns wort
Enzyme inhibitors (ME-DICK-VAG)
Metronidazole
Erythromycin
Disulfiram
INH
Cimetidine
Ketoconazole
Valproic acid
Acute alcoholism
Grapefruit juice
Phenobarbital (enzyme inducer) when given to a patient on chronic warfarin is classified as
Pharmacokinetic antagonist
Constant AMOUNT per unit of time is metabolized
Elimination rate - Rate does NOT increase as drug concentration increases- concentration independent
Halflife = conc Dependent
Zero- order kinetics
Constant FRACTION per unit time is metabolized
Elimination rate- Rate increases as drug concentration increases - concentration dependent
Halflife = conc Independent
First order kinetics
Drugs with Zero order kinetics: (WHAT-PET)
Warfarin
Heparin
Aspirin
Theophylline
Phenytoin
Ethanol (alcohol)
Tolbutamide
Time it takes for drug concentrations to decrease by one half
Half life (t1/2)
Non- linear on semilog paper
Aka: saturable kinetics, michaelis menten kinetics, capacity limited kinetics
Zero order kinetics
Linear on semilog paper
First order kinetics
Removal of drug from the system
Excretion
Volume of blood cleared of drug in unit time
Renal clearance
Competes with active tubular secretion of penicillin, thus, decreases the excretion of penicillin
Probenecid
Doxycycline excreted thru?
Intestinal excretion
Anticancer drugs and teratogenic drugs excreted thru?
Mammary excretion
Mediates inflammation
Prostaglandin
Parent compound of prostaglandin
Cholesterol
———> arachidonic acid
—–> COX (PGG > PGH) / LOX / EPOX
Vasodilator prostaglandins
PGE and PGI
COX 3 inhibitor
Paracetamol
Only IRREVERSIBLE inhibitor of COX
Aspirin
Mostly used as anti platelet
Aspirin 80mg OD
Propionic acid derivatives
-profen
Ibuprofen
Ketoprofeb
Flurbiprofen
Ibuprofen + aspirin = ?
Therapeutic duplication so avoid that!
Flurbiprofen is a long duration profen with adverse reactions such as?
Severe gastric irritation
Myocardial infarction!
Only non acid derived nsaids?
Nabumetone — ketone
Used in post op therapy as substitute for Morphine
Etodolac
Ketorolac
Sulfa drug adverse effect?
SJS!
Inhibits phospholipase A2
Used for closure of PDA
Indomethacin
COX 2 selective drugs that were phased out? Why?
Lumiracoxib
Valdecoxib
Rofecoxib
Because it causes MI and HTN — thrombus formation
Arthritis — due to wear and tear of joints and obesity
Osteoarthritis
Arthritis — due to autoimmunity (WBCs, TNF-a destroy joints and joint destruction due to chemotaxis
Rheumatoid arthritis
Arthritis— hyperuricemia (uric acid rich in bagoong, patis, alcohol, animal liver
Gouty arthritis
Osteoarthritis hallmark in radiograph?
Synovial fluid?
Osteophyte formation
Transparent
Yellowish
Viscus
200 - 1000 WBC — non inflam
Morning stiffness
Improves with movement
Inflammatory arthritis — rheumatoid arthritis , psoriatic or crystal induced arthritis
Pannus formation
Pathogenesis driven by T lymphocytes
Rheumatoid arthritis
Tophi mc involved joint?
Uric acid formation
Gouty arthritis
1st metacarpophalyngeal joint - lowest temperature —– podagra
Main treatment in rheumatoid arthritis
DMARDs – againts chemotaxis
Supplement with NSAID for pain
Glucocorticoids for severe pain
MOA of DMARDs
ADR?
Immunosuppression
ADR - immunocompromised
Example of DMARDs
Methotrexate
TNF alpha blockers - inflixiMAB, adalizuMAB, etanercept (receptor blocker)
Abatacept MOA and ADR?
MOA: target CD80 and CD86
ADR: URTI
A BATA — 80 AND 86
Azathioprine MOA?
Inhibits DNA synthesis by affecting INOSINOC ACID (essential in DNA synthesis)
***Cyclophosphamide
Alkylating agent
ADR: leukopenia, NDV, hemorrhagic cystitis
Rescue drug - MESNA
CyclospoRINe
Targets calcineuRIN
ADR: Hirsutism and gingival hyperplasia
Chloroquine/ hydrochloroquine
Antimalarial drug
MOA: unknown
ADR: ocular toxicity and prolongation of QT interval
*** Leflunomide
Inhibits DIHYDROOROTATE DEHYDROGENASE therefore DNA synthesis is inhibited
ADR: GI toxicicty, hepatotoxicity
***Methotrexate
Current DMARD of Choice!!!
Inhibit FOLATE Synthesis by inhibiting AICAR Ttransformylase, **Thymidilate synthetase and **dihydrofolate reductase
ADR: mucositis/mucosal ulcer
Rescue drug: FOLINIC ACID/LEUCOVERIN
Mycophenolate mofetil
not an antifungal!!!
Inhibits CMP
ADR: aplastic anemia
Sulfasalazine
Metabolite: SULFAPYRIDINE
ADR: Allergy – SJS
TNF alpha blockers
MOA: inhibits TNF alpha
ADR: reactivation of Tuberculosis
DOC for acute attack of gout?
COLCHICINE
MOA: inhibit TUBULIN (for WBC migration)
Short duration of action
ADR: diarrhea, GI disturbance, hepatotoxic, nephrotoxic
Drugs that decrease uric acid
Allopurinol
Febuxostat
Probenecid
Sulfapyrazone
Allopurinol
Xanthine oxidase inhibitor
Metabolite : allocanthine
Purine –XO—-> uric acid
Febuxostat
First NON PURINE XANTHINE OXIDASE inhibitor
Probenecid and sulfapyrazolne
Inhibit reabsorptiin of uric acid in *PCT — *URICOSURIC AGENT
Note— ***** PROBENECID and PENICILLIN — Prolongs the action of penicillin
* probenecid prevents tubular active reabsorption of penicillin
Standard prophylactic antibiotic class for colon sx
2nd gen Cephalosporin (Cefotetan & Cefoxitan)
- combines Gram neg and anaerombe coverage
Standard prophylactic antibiotic for gastric surgery
1st Gen cephalosporin (Cephazolin)
Antibiotic of choice for Gram positive becteremia in inpatient setting
Vancomycin bec MRSA for inpatients until sensitivities are available