Pharm Test 1

Found in the blood plasma an enzyme that breaksdown succinylcholine

Antidote for non-deploarizing NMJ blocking agents

Depolarizing blocker (non-competitive)

Non-Depolarizing Blocker (competitive)

Non-Depolarizinf Blocker (Competitive) 

Used in surgery to promote skeletal muscle relaxtion. intubation, main controlled ventilation, paralysis of skeletal muscle in area of surgery.

Synthesis, Storage, Release, Recognition, Metablosim 

Insectidices (malathion, parathion, diazinon) Nerve Gases (sarin, soman, tabun)

Very short acting used for diagnosis of myasthnia gravis 

Dose not penetrate CNS used to treat myasthnia gravis

Tx poisioning with muscarinic agent. Penetrates CNS

• Dry as a bone
• Hot as a Pistol
• Red as a beet
• Blind as a bat
• Mad as a hatter

• Anitmusacarnic
• Belladona Alkaloids
• Pre-op to reduce salivation/bronchial secretions, reduce intestinal motiltiy, treat overactive bladder, used for opthalmolgical examinations mydriasis, prevent motion sickness, tx asthama, treat AChE inhibitor poisioning

No nicotinic effect, Orally treat sjogren's syndrome (difficulty with salivation and sweating)

No nicotinic effect, somewhat selective for urinary bladder, orally for treatment of post-op urniary retention

No nicotinic effects selective to salivary glands, tx of xerostomia, topically to tx glaucoma. Adverse effect over stimulation of muscarinc receptors

• Absorption
• Distrubution 
• Elimination (clearance)

Transfer of drug from site of action to systemic circulation

Transfer of drug from systemic circulation to tissue

• Removal of the drug from the body
• Metabolism mainly by the liver and excretion through renal or hepatobiliary

Passive Diffusion: Low molecular weight drugs that are both water a lipid soluble dissolve in membrane and cross to the other side

Pka: is the pH at which half of the drug is in its ionized form. 50% charged and 50% uncharged

• Filtration
• Transport Mechanisms: Facilitated Diffusion and Active Transport

Filtration

Facilitated Diffusion

Active Transport

Bioavailabilty

• Reduced by 1st pass effect 
• Altered by chenges in GI motility 
• Can be reduced by other substances present in the GI tract (antacids inhibit absorption of tetracyclines)

• Protein bound drug cannot distribute to tissues or be elminated.
• Bound drug is pharmacologically inactive
• Only free unbound drug is available for Distribution to sites of action and for Elimination. 
• One drug can displace another from binding site (causing a drug drug interaction)

• Blood Flow (ie. stroke pts has decrease blood flow)
• pH differences b/w plasma and intracellular barrier
• Specialized barriers: Blood-Brain Barrier
• Tissue factors affecting accumulation or binding of drug (ie. edema)

The Cytochrome P450 system (CYP) and it is found in the Liver

Biotransformation

In the liver and by the CYP P450

(nonsynthetic) Oxidation Reduction Reaction by Oxygenases and Reductases

(Synthetic) Formation of conjugates by Tranferases; drugs are conjugated with a sugar an amino acid or sulfate. Phase 2 drugs are easier to metabolize

• Metabolite is more water soluble
• Metabolite may be less active
• Metabolite may be more active: -Prodrug: INACTIVE DRUG UNTIL CONVERTED TO ACTIVE FORM BY THE BODY
• Metabolite may be inactive
• Metabolite may be less toxic
• Metabolite may be more toxic 

by alkalinizing the urine

Bicarbonate or Diuretic Acetazolamide which increase bicarb in the urine

Acidify the Urine

Ammonium Chloride

drug conjugate secreted into the bile and reconverted to parent compound by intestinal bacteria can be reabsorbed from small intestines-Recycling (Can extend the duration of the drug in the body)

Contant Percentage of drug eliminated per unit time

Time necessary to reduce plasma drug levels by one half. 

Constant amount of drug eliminated per unit time (ie. 50mg/4hr)

Regulatory proteins that interact with a drug or hormone and initiate a cellular response

How well the drug binds (STRENGTH/LOVE). Drugs that interact with receptor to prduce a response

The capacity of a drug to produce a response after it binds

Has Affinity and Efficacy

Has ONLY Affinity

Can produce full response; Efficacy=1

Produce a response less that that of a full agonist; Efficacy >0 but <1

Produce a response less than that of a full agonsist; Efficacy<0

• Have Affinity
• Have NO Efficacy
• Block the binding by an agonsit to its receptor
• Blockade can be OVERCOME (SURMOUNTABLE)
• Reduce the Potency of agonist

• Have Affinity
• Have NO Efficacy
• Block the binding by an agonsit to its receptor
• BLOCKADE CANNOT BE OVERCOME
• Reduce the Efficacy of Agonist

Can only prevent so much of the agonist from binding can't shut off site completely but can only modulate it. Causes the protein to change shape so the agonsit can't bind

• Muscarinic Recptors
• Salivation
• Lacrimation
• Urination
• Defecation
• Emesis

• INCREASE contractile force
• Increase HR (TACHYCARDIA)
• Increase Renin Release

DECREASE vasodilation and TPR (bronchorelaxation, mydriasis, decreased urination and GI motility, utureus relax)

INCREASE Vasoconstriction and TPR

DA, B1, A1. Increase UO 

A1 A2 and B1

• A1 A2 B1 B2
• Tx Asthma 
• Anaphylatic Shock
• Cardiogenic Shock
• Prolong action of local anesthetics
• Topical hemostatic agent

• Tx CHF
• DA B1 A1

• 1. Pheneylephrine (a1)
• 2. Methoxamine (a1)
• 3. Oxymetazoline (a1 and a2 in periphary)
• 4. Tetrahydrozoline (a1)
• 5. Nephazoline (a1)
• 6. Ephdrine/Pseudoephedrine (a1)
• 7. Clonidine (a2, Tx site of action is the CNS)

Isoproterenol Tx CHF increase pulse no change in MAP

• 1. Albuterol
• 2. Terbutaline
• 3. Metaproterenol
• Bronchodilators inhaled agents. can decrease BP and increase HR cause syncope. *B2 is important on arterioles

Dobutamine tx CHF increase CO

• Clonidine (a2 agonist) Antihypertensive.
• Initially it increase BP but cross BBB it decrease BP can cause sleepiness and no ejaculation. it contracts vessels barroreflux do not work because it decreases HR and BP

Phentolamine 

• Prazosin (drug of choice for A1) Terazosin (water soluble don't block A2 in the brain)
• Used tx as antihypertensive agents

• OLOL
• NonSelective B1 and B2 Propanolol Pindolol Timolol Nadolol
• Selective B1AMA= Atenolol Metropolo Acebutolol (B1 went to the AMA)
• Nonselective B1 B2 A1 Carvedilol Labetalol

• Tyramine (dieatry substance)
• Ephedrine
• Pseudoephedrine
• Amphetamine
• influenece nerve terminal release of NE binds to alpha and beta

• Cocaine
• Tricyclic Antidepressants

Guanethadine

Reserpine

• Pargyline
• Tranylcypromine

Tyramine (or other drugs that promote NE release) may cause markedly increased BP in patients taking MAO inhibitors