Term
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Definition
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Term
|
Definition
Cholinomimetic
Choline Ester |
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Term
|
Definition
Cholinomimetic
Choline Ester |
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Term
|
Definition
Cholinomimetic
Choline Ester |
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Term
|
Definition
Cholinomimetic
Choline Ester |
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Term
| SAR of Choline Esters (3 parts) |
|
Definition
Quaternary ammonium (N wth a positive charge)
Acyloxyl Group (preferably an ester for Hydrogen bonding)
2 carbon unit beta the Oxygen and the Nitrogen |
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Term
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Definition
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Term
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Definition
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Term
|
Definition
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Term
|
Definition
Cholinomimetic
Alkaloid (M1 agonist) |
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Term
|
Definition
Cholinomimetic
Alkaloid (M1 agonist) |
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Term
|
Definition
| All have basic Nitrogenous atoms |
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Term
|
Definition
| Reversible AchE inhibitor |
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Term
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Definition
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Term
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Definition
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Term
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Definition
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Term
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Definition
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Term
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Definition
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Term
|
Definition
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Term
|
Definition
| Reversible AchE inhibitor |
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Term
| Chemical Structure of AchE inhibitors |
|
Definition
| they all contain an aromatic ring |
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Term
|
Definition
| Irreversible AchE inhibitor used as Drug |
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Term
|
Definition
| Irreversible AchE inhibitor used as Drug |
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Term
|
Definition
| Irreversible AchE inhibitor used as insecticide |
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Term
|
Definition
| Irreversible AchE inhibitor used as insecticide |
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Term
|
Definition
| Irreversible AchE inhibitor used as chemical warfar agent |
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Term
|
Definition
| Irreversible AchE inhibitor used as chemical warfar agent |
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Term
|
Definition
| Cholinesterase Reactivator |
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|
Term
| Chemical structure of irreversible AchE inhibitors |
|
Definition
| all contain a P (organophosphates), they phosphorylate the active site |
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Term
|
Definition
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Term
|
Definition
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Term
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Definition
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Term
|
Definition
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Term
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Definition
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Term
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Definition
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Term
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Definition
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Term
|
Definition
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Term
|
Definition
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Term
|
Definition
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Term
|
Definition
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Term
|
Definition
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Term
|
Definition
| Selective Muscarinic Antagonist (M1 selective antiulcer drug) |
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Term
|
Definition
| Selective Muscarinic Antagonist (M1 selective) |
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Term
|
Definition
| Selective Muscarinic Antagonist (M2 selective) |
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Term
|
Definition
| Selective Muscarinic Antagonist (M2 selective) also a neuromuscular blocking agent. |
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Term
|
Definition
Nicotinic Antagonist
Neuromuscular Blocking Agent
Depolarizing Agent |
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Term
|
Definition
Nicotinic Antagonist
Neuromuscular Blocking Agent
Depolarizing Agent |
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Term
|
Definition
Nicotinic Antagonist
Neuromuscular Blocking Agent
Specific Nondepolarizing Agents |
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Term
|
Definition
Nicotinic Antagonist
Neuromuscular Blocking Agent
Specific Nondepolarizing Agents |
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Term
|
Definition
Nicotinic Antagonist
Neuromuscular Blocking Agent
Steroid Based Agents |
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Term
|
Definition
Nicotinic Antagonist
Neuromuscular Blocking Agent
Steroid Based Agents |
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Term
|
Definition
Nicotinic Antagonist
Neuromuscular Blocking Agent
Steroid Based Agents |
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Term
|
Definition
Nicotinic Antagonist
Neuromuscular Blocking Agent
Steroid Based Agents |
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Term
|
Definition
Nicotonic Antagonist
Neuromuscular Blocking Agent
Tetrahydroisoquionolone based agents |
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Term
|
Definition
Nicotonic Antagonist
Neuromuscular Blocking Agent
Tetrahydroisoquionolone based agents |
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Term
|
Definition
Nicotonic Antagonist
Neuromuscular Blocking Agent
Tetrahydroisoquionolone based agents |
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|
Term
| Biologically most important PGs |
|
Definition
| PGE's, PGF's, PGI, and Thromboaxanes |
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Term
|
Definition
|
|
Term
| metabolic intermediates of PGs |
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Definition
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|
Term
| SRS-A's (slow reactive substances of anaphylaxis) |
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Definition
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|
Term
|
Definition
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|
Term
| Side effects of NSAIDS (2) |
|
Definition
GI irritation (due to inhibition of PG synthesis which produces a protective effect on the GI)
Prolongation of bleeding time due to inhibition of TxA synthesis |
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Term
|
Definition
| Inhibit Phospholipase A2 (reduce the amount of free arachidonic acid that is available for PG and LTE synthesis) |
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Term
| Corticosteroids + Receptor in cytosol= |
|
Definition
| Limodulin which inhibits Phospholipase A2 |
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Term
| Resistance to Corticosteroids (2 cases) |
|
Definition
cells with abundance of AA
cells with no protein synthesis (platelets) |
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|
Term
| Cardiovascular: PGs that cause vasodilation |
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Definition
|
|
Term
| PG's involved in maintaining patency of Ductus Arteriosus |
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Definition
|
|
Term
|
Definition
| shunts blood away from the lungs in the fetus. begins to degrade after birth. A PG can be administered if it is neccessary to maintain the DA |
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|
Term
| potent inducer of platelet aggregation and synthesized by platelets |
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Definition
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|
Term
| Drug that helps prevent platelet aggregation in cerebrovascular system |
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Definition
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|
Term
| PG that relaxes bronchial smooth muscle |
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Definition
|
|
Term
| Luekotrienes cause _______________ in Bronchial Smooth Muscle |
|
Definition
| Bronchoconstriction (SRS-A) |
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|
Term
| PG's that contract a pregnant uterus later in pregnancy |
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Definition
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|
Term
| Major obstacle to therapeutic use of PG's is that the contract the ____________ |
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Definition
| intestine (causing nausea, vomiting, diarrhea) PGE's and PGF's |
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|
Term
| PG that causes pain and irritations |
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Definition
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|
Term
| PG that sensitizes nerve endings |
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Definition
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|
Term
| PG's involved in inflammation |
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Definition
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Term
| PG administered vaginally to induce therapuetic abortions during 2nd trimester ALSO can be used for cervical ripening in labor induction |
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Definition
| PGE2 (Dinoprostone aka Prostin E2 and Cervidil) |
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Term
| PG used in the treatment of Erectile Disfunction |
|
Definition
| PGE1 (Alprostadil aka Caverject), causes vasodilation of the cavernosa |
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Term
| PG used to reduce platelet aggregation in a blood transfusion |
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Definition
|
|
Term
|
Definition
| used by continous IV infusion to produce a relaxation of smooth muscle. |
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Term
| Pg used to maintain Ductus Arteriosus in congenital heart diseas defect prior to durgery |
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Definition
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Term
|
Definition
| used as a cytoprotective agent in patients on longh term NSAID therapy (synthetic analog of PGE1) |
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Term
|
Definition
| Used in Glaucoma, by causing an increased outflow of aqueous humor lowering intraocular pressure in open angle glaucoma. Long acting stable PGF2 derivative, admin as gtts bid. WILL CHANGE EYE COLOR TO BROWN EVENTUALLY. |
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Term
| True/False: COX is the enzyme required for leukotriene byosynthesis |
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Definition
|
|
Term
| T/F PGG is considered a metabolic intermediate in PG biosynthesis |
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Definition
|
|
Term
| T/F: Aspirin is the most potent inhibitor of PG biosynthesis |
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Definition
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Term
| T/F: Steroids inhibit both PG and LTE biosynthesis |
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Definition
| True because they inhibit PLA2 |
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Term
| T/F: PGE1 and protacycline are responsible for SRS-A |
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Definition
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Term
| T/F: Latanoprost (Xalatan) is used to prevent GI irritation caused by NSAIDS |
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Definition
| False: Ltanoprost is used as a treatment for glaucoma to increase outflow of aqueous humor. it is a PGF2 derivative |
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Term
| T/F: Aloprostadil is a PGE1 derivative used to harvest platelets. |
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Definition
|
|
Term
| T/F: No specific receptors for the PG's have been identified |
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Definition
| False, there is EP, FP, DP, IP, and TP |
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Term
| 3 classes of Adrenal Steroids |
|
Definition
1. Glucocorticoids
2. Mineralocorticoids
3. Gonadal Steroids |
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|
Term
| Side effect of high levels of glucocorticoids |
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Definition
|
|
Term
| pertaining to Ca metabolism, glucocorticoids cause: |
|
Definition
| decreased Ca absorption and increased Ca excretion in urine. |
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|
Term
| Action on Blood Cells: Glucocorticoids cause |
|
Definition
| decrease in circulating Eosinophils, lymphocytes, neutrophils, and basophils, atrophy of lymphoid tissue. RESISTANCE TO INFECTION IS DECREASED |
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Term
| T/F: Glucocorticoids have an antiinflammatory and immunosuppresive action |
|
Definition
| True: inhibits PLA2 but also decreases lymphoctes and macrophages |
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Term
| Glucocorticoid CNS effect |
|
Definition
| mental depression and irritability |
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|
Term
| T/F: Glucocorticoids stimulate ACTH |
|
Definition
| False, they inhibit ACTH leading to adrenal atrophy |
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Term
|
Definition
Na and H20 retention
K and H loss |
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|
Term
| Mineralocorticoids act on |
|
Definition
| distal tubules and collecting ducts of the kidneys |
|
|
Term
| glucocorticoids are tightly bound to plasma globulin: |
|
Definition
| Transcortin and Coriticosteroid Binding Globulin (CNG) |
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|
Term
| T/F: CGG has less affinity for synthetic steroids (Dexamethasone) |
|
Definition
| True: could explain their e=increased potency. |
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|
Term
| Primary adrenal insufficiency |
|
Definition
| decreased glucocorticoid and mineralocorticoid secretion |
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|
Term
| Secondary Adrenal Insufficiency |
|
Definition
| Lack of CRH released from hypothalamus or lack of ACTH produced by pituitary |
|
|
Term
| Congenital Adrenal Hyperplasia |
|
Definition
| overproduction of testosterone (ambiguous genitalia) |
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Term
| Contraindications and Precautions for glucocorticoids |
|
Definition
1. agitated psychotic state (because it can cause metal depression)
2. Active peptice ulcer (causes acid secretion)
3. Diabetes (causes an increase in blood glucose levels)
4. Osteoporosis because of gluconeogenesis
5. Hypertension because of Na retaining steroid
6. Infection, can cause immunosuppresion but can also mask signs of infection |
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|
Term
| Aminoglutethimide (Cytadren) |
|
Definition
| Inhibits synthesis of all the steroid, could be used to treat an adrenal tumor which would cause increased stimulation and secretion of steroids. |
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Term
| Spironolactone (Aldatone) |
|
Definition
| Mineralocorticoid receptor antagonist. Structure very similar to testosterone and aldosterone (competes for receptor) used to treat hirsuitism. Also as a short acting K sparing diuretic |
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Term
| T/F: common gonadaol steroids such as estradiol and testosterone are produced by the adrenal cortex |
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Definition
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|
Term
| T/F: treatment with dexamethasone would cause a rapid increase in the level of lymphocytes and neutrophils in the circulations |
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Definition
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|
Term
| T/F: Synthetic glucocorticoids have a much lower affinity for CBG than endogenous glucocorticoids |
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Definition
|
|
Term
| T/F: Primary Adrenal insufficiency is due to the lack of ACTH secretion from the anterior pitutary |
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Definition
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|
Term
| T/F: Aminoglutehtimide(Cytadren)is used in the treatment of Cushings Disease |
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Definition
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|
Term
| T/F: Spirinolactone has a chemical structure similar to testosterone |
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Definition
|
|
Term
|
Definition
| Prostaglandins, Prostacyclines, and Thromboxanes |
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|
Term
| Thromboxanes have a ________ membered ring |
|
Definition
|
|
Term
| Arachidonic Acid is acted upon by what enzyme |
|
Definition
|
|
Term
| Version of COX that causes inflammation |
|
Definition
|
|
Term
| NSAID Binding Site on COX1 |
|
Definition
| Isoleucine at position 523 |
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|
Term
| NSAID binding site on COX2 |
|
Definition
|
|
Term
|
Definition
| 2 cyclic 5 membered ring structures |
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|
Term
| 1st metabolic reaction of PG's |
|
Definition
| oxidation at C15 of the allylic alcohol-can be easily oxidized because of its proximity to a double bond |
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|
Term
| 2nd step in PG metabolism |
|
Definition
| Reduction of double bond between C13 and C14 |
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|
Term
| 3rd step in PG metabolism |
|
Definition
| Beta Oxidation starting at C1 to form nor-prostaglandins |
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|
Term
| 4th step in PG metabolism |
|
Definition
| Omega oxidation starting at the alkyl end (C20) |
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|
Term
| Latanoprost structural differences are |
|
Definition
| PGF2 derivative: has a benzene in place of C20 and an ester in place of COOH at C1 |
|
|
Term
|
Definition
| stereochemically crowd the OH at C15 to prevent oxidase enzyme from oxidizing the OH and setting of subsequent metabolic reaction |
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|
Term
|
Definition
| Latanoprost (PGF2 derivative) |
|
|
Term
|
Definition
| misoprostol aka Cytotec (PGE1 analog) cytoprotective agent in pts on long term NSAID therapy |
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|
Term
|
Definition
|
|
Term
|
Definition
| epoprostenol (Flolan) is a prostacyclin treatment for severe hypertension relaxes vascular smooth muscle. must be given IV |
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|
Term
|
Definition
|
|
Term
|
Definition
| alprostadil (PGE1 derivative) used in erectile disfunction and also to prevent platelet aggregation in blood transfusions |
|
|
Term
|
Definition
| CPPP (cyclopentanoperyhydrophenanthrene) three benzene rings followed by a 5 membered cyclic structure |
|
|
Term
| Most steroids are in what configurations |
|
Definition
|
|
Term
| Steroids: if double bond is in either ring A or B and is between C5 and C6 |
|
Definition
|
|
Term
| Steroids: Double bond is in either ring A or B and is between C4 and C5 |
|
Definition
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|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
| All classes of steroid are in the ___________ configuration except bile acids and cardiac glycosides |
|
Definition
|
|
Term
| Estranes have ________ Carbons |
|
Definition
|
|
Term
| Androstanes have _______ Carbons |
|
Definition
|
|
Term
| Pregnanes have ___________ Carbons |
|
Definition
|
|
Term
| 6 carbon compound that is acted upon by HMG-CoA reductase to produce mevalonic acid |
|
Definition
| Beta-hydroxy-Beta methylgutaryl CoA. |
|
|
Term
| It is likely to prevent the formation of cholesterol by inhibiting what enzyme? |
|
Definition
| HMG-CoA reductase which will stop the conversion of acetate to mevalonic acid |
|
|
Term
| Important difference between mineralocorticoids and glucocorticoids |
|
Definition
| mineralocorticoids do not have OH group at C17 attached by enzyme 17alpha hydroxylase |
|
|
Term
| Mineralocorticoids and glucocorticoids both have a __________ group at C3 |
|
Definition
|
|
Term
| Prednisolone group modified at: |
|
Definition
| C1-C2=double bond, Add OH or CHS at C16 |
|
|
Term
| Substituents which significantly increase anti-inflammatory and glucocorticoid activity |
|
Definition
| 1-dehydro and 6alpha-fluoro |
|
|
Term
| Substituents that signicantly decrease mineralocorticoid activity |
|
Definition
| 16alpha-hydroxy, 16alpha and 18Beta methyl, 16alpha and 17alpha ketals |
|
|
Term
| Substituents which signifcantly increase both gluococorticoid and mineralocorticoid activites |
|
Definition
| 9alpha-fluoro, 21-hydroxy, 2alpha methyl, 9 alpha chloro |
|
|
Term
| Goal of adrenocorticoid drug |
|
Definition
| compounds with high gluco and low mineralocorticoid activity |
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|
Term
| agents that compete for binding to steroid receptors |
|
Definition
| Adrenocorticoid Anatgonists (Sprinolactone and derivative of 19-nortestosterone) |
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|
Term
|
Definition
| Testosterone production occurs here |
|
|
Term
| Seminiferous Tubule and Sertoli Cell |
|
Definition
| Spermatogenesis occurs here. |
|
|
Term
| LH stimulates ___________ in males |
|
Definition
| testosterone production in Leydig Cells |
|
|
Term
| FSH stimulates _____________ in males |
|
Definition
| spermatogenesis in seminiferous tubules |
|
|
Term
| what enzymne converts testosterone to estradiol? |
|
Definition
| aromatase (turns 5 membered cyclic ring into a aromatic ring) |
|
|
Term
| What enzyme converts Testosterone to Dihydrotestosterone |
|
Definition
|
|
Term
| T/F Testosterone administered orally is rapidly absorbed but metabolized in the liver and is thus not effective |
|
Definition
|
|
Term
| Testosterones esters are administered ________ and absorbed slowly for sustained activity |
|
Definition
|
|
Term
| What can be done to prevent oral testosterone from being metabolized in the liver by oxidation |
|
Definition
|
|
Term
| 98% of testosterone is bound to ___________________ |
|
Definition
| (sex hormone) binding globulin. |
|
|
Term
| Methyltestosterone (Virilron) |
|
Definition
|
|
Term
|
Definition
|
|
Term
| anabolic steroid ratio of anabolic to androgenic |
|
Definition
|
|
Term
| Drug: Gonadotropin releasing hormone: Leuprolide |
|
Definition
| (synthesis inhibitor) Inhibits LH secretion which leads to a reduction in testosterone production and release. used in prostatic cancer |
|
|
Term
|
Definition
| 5alpha reductase inhibitor. greatly reduces the conversion of testosterone to dihydrotestosterone. used primarily for BPH and male pattern baldness |
|
|
Term
| In females: Estrogens produce a protective effect on ________ and the _____ system |
|
Definition
|
|
Term
|
Definition
| Selective estrogen receptor modulators; act at the estrogen receptor site and produce modulate estradiol activity |
|
|
Term
| necessary for complete sexual development, menstrual cyle, and pregnancy. actions are secondary to estrogen |
|
Definition
|
|
Term
| ER found in reproductive tissue |
|
Definition
|
|
Term
| ER found in Bone and CV systen |
|
Definition
|
|
Term
| T/F: synthetic estrogens are not orally active |
|
Definition
| FALSE, they are resistant to metabolism making them ORALLY ACTIVE |
|
|
Term
|
Definition
| Sulfated ester of estrone (conjugated estrogens) |
|
|
Term
| Adverse side effects of estradiol |
|
Definition
| nausea (common), fluid retention. CV events, breat cancer, and chloasma |
|
|
Term
|
Definition
| antiestrogen; SERM used for breat cancer. provides mixed (agonist and antagonist) activity |
|
|
Term
|
Definition
| SERM selective agonist for ER beta (bone and CV)/selective antagonist for ER alpha-reproductive tissue. used to treat or prevent postmenopausal osteoporosis |
|
|
Term
|
Definition
| Estrogen Synthesis Inhibitor, inhibits aromatase. used in advanced treatment of breast cancer and cancer metastasis following Tamoxifen |
|
|
Term
|
Definition
| Progestin; good oral activity- used in oral contraceptive |
|
|
Term
|
Definition
| anti-progestin; 11 Beta substitued derivative of norethindrone. Acts as a competitive receptor antagonist-medical abortions by preventing implantation of fertilized ovum. |
|
|
Term
| T/F:Testosterone is secreted from the Sertoli Cells |
|
Definition
|
|
Term
| T/F: Testosterone is absorbed by the oral route of administration but is pharmacologically inactive |
|
Definition
|
|
Term
| T/F: In most target tissues, testosterone must be metabolized to dihydrotestosterone in order to produce a biological response |
|
Definition
|
|
Term
| T/F: Testosterone is responsible for the closure of the epiphysis in males |
|
Definition
|
|
Term
| T/F: Flutamide is a steroid which inhibits 5 alpha reductase activity |
|
Definition
|
|
Term
| T/F: Anabolic Steroids act on the same receptor as testosterone |
|
Definition
|
|
Term
| T/F: Estrogens have an aromatic A Ring |
|
Definition
|
|
Term
| T/F: Gonadotropins are secreted in a pulsitile manner |
|
Definition
|
|
Term
| T/F: Estradiol reacts with a cytoplasmic receptor to increase intracellular cyclic AMP |
|
Definition
|
|
Term
| T/F: Anastrozole (Arimidex) competes with estradiol for ER binding |
|
Definition
| False: aromatase inhibitor |
|
|
Term
| T/F: Progesterone acts at the estrogen receptor |
|
Definition
| False: has own receptor PR |
|
|
Term
| T/F: The PR is a membrane bound receptor |
|
Definition
|
|
Term
| T/F: Progestorone acetate (Cyclin) has very good oral activity |
|
Definition
| False: has poor GI absorption |
|
|
Term
| T/F: RU-486 (Mifepristone) inhibits the biosynthesis of progesterone |
|
Definition
| False: Competetive receptor antagonist. |
|
|
Term
| Two principal classes of female sex hormones: |
|
Definition
|
|
Term
|
Definition
| Induce estrus in various mammalian species and bring about secondary sex characteristics in females |
|
|
Term
|
Definition
| perform important functions in the reproductive system and serve as precursors to androgens, estrogens, and adrenocorticoids |
|
|
Term
|
Definition
| Important precursor to both families of sex hormones |
|
|
Term
|
Definition
1. Aromatc A ring
2. Phenolic OH at C3
3. 17beta OH
4. Distance between the two OH groups is 8.55 angstroms
5. Planar hydrophobic molecule due to aromatic A ring |
|
|
Term
|
Definition
| compound that in excess will sit at the receptor and prevent androstenedione from coming in or prevent estradiol from coming in (estriol bc of 3 OH's) |
|
|
Term
| Triphenylethylene antiestrogens |
|
Definition
| 3 benzene rings sitting on a 2 carbon unsaturated spacer. (ex:tamoxifen) |
|
|
Term
|
Definition
| compounds that do not have estrogenic properties. |
|
|
Term
|
Definition
|
|
Term
| Most abundant pregnane steroid in urine during pregnancy |
|
Definition
| 5 beta pregnandiol glucoronide |
|
|
