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What is a Drug
Something that causes physioological changes in an organism when administered
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What kind of a mixture are most drugs
Racemic
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What is pharmacokinetics
This is what the body does with the drug (absortion, distribution, biotransformation, and elimination)
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What are three ways that a drug can be classified
- Main effect
- Clinical and therapeudic use
- Mechanism of action
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What are the different routes for drug administration
Enteral and parenteral
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What is the enteral route of a drug
This is when the drug enters the body through the GI tract is some way
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What is the parenteral route of a drug into the body
This is when the drug enter the body by any route but the GI tract
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What is used for the quantatative measurement of a drug
The volume of drug distribution VD
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What are the two ways that a drug is removed from the body
- Biotransformation
- Excretion
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What is the most important route for drug excretion
Renal excretion
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Metabolism or biotrasformation of a drug means
The conversion of a drug into a different substance, This can activate the drug, deactivate the drug, or maintain the drugs activity
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What is the most important organ involved in drug metabolism
Liver
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What is a major enzyme of drug metabolism found in the smooth ER of the liver
cytochrome P450 (CYP) enzymes
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What is pharmacodynamics
What the drug does to the body
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The molecular target for a drug is called
Drugs receptor
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Most of the drug receptors in the body are
Macromolecules which are proteins most of the time
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Some examples of drug receptors that are proteins are
Regulatory proteins, ion channels, enzymes, carrier proteins, and structural proteins
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A single drug may have more then one
Receptor and can therfore effect them in different ways and degrees
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What are the different classes of drugs based on effect and function on a receptor
- Agonist (Either initiates or decreases the activity)
- Antagonist (Prevents any activation of the receptor)
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What is a pharmacological action
The observed effect which has been produced by the drug
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Theoretically drugs can be divided into what two groups of pharmacological effects
- Drugs targeting self
- Drugs targeting non-self (like bacteria, viruses, ect)
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What is Toxicology
The study of the adverse affects of drugs
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What is Contraindictions
A condition that makes the drug inadvisable
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What is an Autacoid
Any chemical substance that is able to transmit signals between cells
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What are the three main classes of Autocoids
- Hormones
- Neurotransmitters
- Autocoids
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What are the general effects of a hormone
- They are secreted directly into the circulation by endocrine organs
- They target distal organs, tissues or cells
- They are typically slow acting
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What are the characteristics of a neurotransmitter
- They are released by neurons
- They target adjacent cells
- Rapid acting
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What are the characteristics of the subclass of Autocoids
- They are local factors (paracrine factors)
- They act in a short range on adjacent cells
- Rapid acting
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What are the major classes of the subclass of Autocoids
- Histamine
- Serotonin
- Endergeneous peptides (Vaso active)
- Eicosinoids (Prostaglandins and leukotrienes)
- Cytokines
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What are the two most important H-1 receptor antagonists up to this point
- 1st generation
- Dimenhydrinate (Dramamine)
- Diphenhydramine (Benedryl)
- 2nd Generation
- Cetirizine (Zyrtec)
- Loratadine (Claritin)
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What are the affects of the 1st generation H-1 receptor antagonists Dimenhydrinate and Diphenhydramine
- They have strong sedative effects
- They block autonomic receptors
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What are the affects of the 2nd generation H-1 receptor antagonists Cetirizine and Loratadine
Less sedation then first generation
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What are the pharmacokinetics of H-1 receptor antagonists
- They are rapidly absorbed after administration (2-3hrs)
- Widely distributed to all the body
- Effects the body for 4-6 hrs in most cases
- They are reversible competitive inhibitors of Histamine receptors
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Why are 1st generation H-1 receptor antagonists better sedatives
They pass the Blood Brain Barrier
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Several 2nd generation H-1 antagonists are metabolized by
The CYP3A4 system
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What kind of receptors do the H-1 antagonist inhibit
G proteins that are stimulated by histamine and that stimulate IP3 DAG2nd receptors
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1st Generation H-1 antagonists besides blocking Histamine receptors can effect
Muscarinic cholinoreceptors, alpha adrenoreceptors, and serotonin receptors
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2nd generation H-1 antagonist, beyond general histamine receptors also inhibit
Histamine receptors specifically in the mast cells and basophils
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What are the pharmacological effects of the H-1 antagonist
Inhibition of Adema, Itching, antinausea, histamine induced hypotension, inhibition of bronchiolar and GI constriction
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Why should caution be taken when trying to sedate a child with 1st generation H-1 antagonists
It has the opposite effect on them
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Which 1st generation H-2 receptor can be a potent local anesthetic when given in high doses
Diphenydramine
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What is prophylactic
Using a drug prior to issue emerging
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What are the mild adverse effects of 1st generation H-1 receptors
Dizziness, fatigue, nausea/vomiting, constipation, diarrhea
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What effects could overdose of H-1 Antagonists have
Hallucinations, convulsions, tachycardia, coma, cardiorespiratory collapse, death
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What are the two H-2 receptor antagonists to remember at this point
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What are the only two routes into the body for Cimitidine and Famotidine (H-2 Antagonists)
Oral and Parenteral (injection)
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What is bioavailability of Cimetidine and Famotidine
50% percent because it is matobolized in the liver
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Does Cimetidine and famotidine pass the BBB
Yes, it circulates to the whole system
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How is Cimetidine and famotidine cleared
Through the combination of hepatic metabolism, glomerular filtration, and renal tubule secretion. For this reason, patients with renal or hepatic issues should be monitored close
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Cimetidine and famotidineneed is to to be used with caution on the elderly because
The clearance of the drug is dimished by 50% as well as the distribution
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H-2 antagonitsts have what pharmacodynamics
They are competetive inhibitors of histamine in the stomach parietal cells, as well as cardiac muscle, mast cells, and the brain
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What specific receptors in the in the cascade are affected by H-2 antagonists
GPCR's which stimulate production of cAMP
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What kind of clinical uses are the H-2 antagonists used for
Gastric reflux disease (GERD), Sour stomach (Dyspesia), and peptic ulcers.
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Ulcers caused by H. Pylori should not be treated with
H-2 Antagonists
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What are the adverse affects of Famotidine and Cinetidine
There are none, only mild affects such as diarrhea, headache, fatigue, ect
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Cimetidine can have an effect on
Dihydrotesterone blockage causing gynecomastia, galactorrhea (sponateous milk production in women), loss of labido, and impotence
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What are the contraindications of H-2 Antagonists
Antacids, cimetidine with drugs that are metabolized by the P450 system (since it will inhibit the effects), use of alcohol
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What is the Triptan Drug to remember and what does it affect
Sumatriptan, serotonin
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Sumatriptan is administered how and has what reaction time
Oral, nasal, parenteral 1-3 hours
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What is the mechanism of action of sumatriptan
It is an agonist for serotonin 5-HT and they mediate vasoconstriction in the brain
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What are the pharmacological uses of Sumatriptan
Migraine headaches (Cluster headaches)
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What is the toxicity of Sumatriptan
- It can alter sensations (tingling, warmth, ect.)
- Dizziness
- Weakness
- Neck pain
- Injection site reactions
- Chest discomfort
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What are the contraindications or Sumatriptan
- Not to be taken with any cardiovascular disease
- Use of other 5H-T agonists
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How are Eicosanoids derived
They are lipid derived autacoids
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What are the two main groups of Eicosanoids
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Prostanoids, a class of Eicosanoids have what two sub classes
- Prostaglandins
- Thromboxanes
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Arachidonic acid (AA) is a poly unsaturated fat that is significant because
- We can't make them
- They are the precursors to Eicosanoids
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The Arachidonic Acid can be synthesized to Eicosanoids by what two important routes
- Cyclooxygenase (COX) pathway
- Lipoxygenase (LOX) pathway
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What are the two main enzymes in the COX pathway
- COX-1 (The body requires these)
- COX-2 (These are for special needs)
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The LOX pathway is specifically for
Leukotrienes
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What are the pharmacodynamics of Eicosanoids
- They are used as Autocoids (Paracrine/ autocrine secretion)
- They bind to G proteins to activate or inhibit cAMP, IP3/DAG, phospholipase C, and Rho GTPase pathways
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What are the pharmacological effects of Eicosanoids
- Increase the synthesis and release of Prostaglandins which affect a rise in body temperature and the hypothalmic set point
- Potent anteriole vasodialators in vascular beds
- Constrictors in pulmonary beds (Bronchioles)
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Eicosanoids are also used in the female and male reproduction system for
- Women- Uterine contractions,
- Men- Enhance penile erection by relaxing smooth muscle in the corpora cavernosa
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Prostaglandis E and F are used in the eye for
Lowering intraocular pressure
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What are the clinical uses of Alprostadil (Eicosanoid)
- Penile injections
- Keeps the ductus arteriosus in neonates open for corrective surgery later
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What are the clinical uses of Dinoprostone (Eicosanoid)
- Synthetic preparation of PGE2
- Stimulate Uterine contractions
- Abortion in 2nd trimester (1/4 are incomplete)
- Labor induction
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What are the clinical uses of Latanoprost (Eicosanoid)
- Eyes drops
- Gluacoma
- Irreversible brown pigmentation of iris and eyelashes
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What are the clinical uses of Eicosanoid inhibitors
- Asthma
- Organ transplant rejection
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What is unique about Latanoprost
It requires metabolism to activate it
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What are the two Eicosanoid Inhibitors
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