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Pharmacology Exam Components: 1.0. General Principles [5 Qs] 2.0. Central Nervous System [4 Qs] 3.0. Autonomic [3 Qs] 4.0. Cardiovascular [4 Qs] 5.0. Local anesthetics [4 Qs] 6.0. Chemotherapy [5 Qs] 7.0. Endocrines/Immunosuppressants [ 2 Qs] 8.0. Analgesics [5 Qs] 9.0. Antihistamines and Autocoids [2 Qs] Total = 34 questions
1.0. General Principles [5 Qs] 1.1. Rx writing, drug laws, and drug abuse 1.2. Toxicity and drug interaction 1.3. Dose response 1.4. Mechanism of action 1.5. Biotransformation 1.6. Absorption, distribution, excretion 1.7. Alternative (herbal) medications
Pharmacology is the study of how substances interact with living organisms to produce a change in function. To protect the consumer and prevent abuse, many governments regulate the manufacture, sale, and administration of medication. In the United States , the main body that regulates pharmaceuticals is the Food and Drug Administration and they enforce standards set by the United States Pharmacopoeia. The FDA categorizes drugs into six schedules (I to VI). The safety and effectiveness of prescription drugs in the U.S. is regulated by the federal Prescription Drug Marketing Act of 1987 . All drugs have two properties that govern their efficacy. First, Pharmacokinetics describes the effect of the body on the chemical (e.g. half-life and volume of distribution), and second pharmacodynamics describes the chemical's effect (desired or toxic ). The pharmacokinetic properties have 4 properties or characteristics (ADME): Absorption - How is the drug absorbed (skin, the intestine, the oral mucosa)? Distribution - How does it spread through the organism? Metabolism - Is the drug converted chemically inside the body, and into whic h substances. Are these active? Could they be toxic? Excretion - How is drug eliminated (through bile, urine, breath, skin)? Finally drugs have a therapeutic index or therapeutic window which is the ratio of desired effect to toxic effect. A drug with a narrow therapeutic index (close to one) exerts its desired effect at a dose close to its toxic dose.
Schedule I: [Use illegal/restricted to research; high abuse potential; no accepted medicinal use in US]. Examples: hallucinogens, heroin, marijuana Schedule II: [Requires prescription; high abuse potential; no refills or verbal orders allowed; some states require triplicate Rx]. Examples: amphetamines, barbiturates, opiates (single entity, some combos) Schedule III: [Requires prescription; moderate abuse potential; max 5 refills/6mo; verbal orders allowed]. Examples: anabolic steroids, dronabinol, ketamine, opiates. Schedule IV: [Requires prescription; low/moderate abuse potential; max 5 refills/6mo; verbal orders allowed]. Examples: appetite suppressants, benzodiazepines, sedative/hypnotics. Schedule V: [Requires prescription or may be OTC with restrictions in some states; limited abuse potential; max 5 refills/6mo; verbal orders allowed]. Examples: opiate or opiate-derivative antidiarrheals and antitussives.
A medical prescription (? ) is an order (often in written form) by a qualified health care professional to a pharmacist or other therapist for a treatment to be provided to their patient. Usually on the prescription is text that identifies the document as a prescription, the name and address of the prescribing provider and any other legal requirement such as a registration number (e.g. DEA #). The symbol "Rx" meaning "prescription" is a transliteration of a symbol resembling a capital R with a cross on the diagonal (? ). Many brand name drugs have less expensive generic drug substitutes that are chemically equivalent. Prescriptions will also contain instructions on whether the prescriber will allow the pharmacist to substitute a generic version of the drug (e.g. substitution permitted). Some prescriptions will specify whether and how many "repeats" or "refills" are allowed; that is whether the patient may obtain more of the same medication without getting a new prescription from the doctor. In the USA, physicians, veterinarians, dentists, and podiatrists have full prescribing power. Each state regulates what (if any) prescription powers members o f the above group are allowed. There are always 3 elements to a prescription (in addition to patient info, doctor info and dsignature): 1. Rx: medication (including dosage) 2. Disp.: dispensing instructions (number of pills) 3. Sig.: patient instructions (how to take)
Parenteral: Intravascular. sterols). subcutaneous goes straight into general circulation and bypasses first pass liver metabolism. This reduces the effective concentration of drug B. blood supply.e. others drugs are activated by the liver.Topical [i. interaction between drugs come to mind (drug-drug interaction). active. Transport mechanisms (passive. anesthetics. such as a cell (cytotoxicity) or the liver. Pharmacokinetics: the body’s effect on a drug. i. Water solubility of drug (hydrophilic.Intrathecal [i. Alternatively. Enzyme inhibition by Drug A would decrease the effectiveness of Drug B. Hence. even water – by itself not toxic – can lead to water intoxication when taken by a human in large enough doses.Intra-nasal [i. or facilitated)Contact time. Drug interactions may be the result of various processes that alter the the pharmacokinetics of the drug (ADME). non-ionized. This system may be affected by either enzyme induction or enzyme inhibition. protonation. interactions may also exist between drugs & foods (drug-food interactions). anesthetics. which may lead to loss of effectiveness of drug B. (4) First -pass hepatic metabolism: For enteral drugs. hence the injections for Diabetics to bypass the enteral route. surface area. or to a substructure. A central concept of toxicology is that effects are dosedependent. Lipid solubility of drug (hydr ophobic.Toxicity is a measure to the degree to which something is toxic or poisonous. Other: . anti-neoplastics] . Bioavailability .Route of Administration Enteral : GI vs Parenteral : Non-GI Enteral: Oral = stomach = intestines = liver (portal circulation) = heart = general circulation = target tissues. Sublingual or Rectal = straight into general circulation and bypasses first-pass liver metabolism. Drug interaction is a situation in which a substance e.drug A influences the absorption of drug B. Sympathetic co-activity. calcitonin for osteoporosis. thus decreasing bioavailability. Pharmacokinetics (ADME) 1. enzyme induction by Drug A would increase the effectiveness of the drug B by increasing its metab olism to its active form. if Drug B is a prodrug. as discussed in the examples below. then enzyme activation is required for the drug to reach its active form. NOTE: drugs destroyed by acid shoul d be taken without food when possible. Usually.drug A inhibits the production of the enzyme metabolising drug B. increasing bioavailabilityIV (intravenous) route of administration bypasses first-pass liver metabolism. Food in the stomach (delays gastric emptying and increases acid production to allow for proper digestion). 2 . ionized or charged). The examples described above may have different outcomes depending on the nature of the drugs.e. tissues. (2) Stability: Insulin is unstable in the GI tract.g. Drug.e.e. Typically. analgesics. drug interactions may be the result of the pharmacodynamic properties of the drug. (3) Permeability: this is determined by pH (acid-base interactions. Metabolism based drug interactions: One notable system involved in metabolic drug interactions is the enzyme system comprising the cytochrome P450 oxidases. The study of poisons is known as toxicology. Absorption: The onset of action of a drug is primarily determined by the rate of absorption Absorption (continued): 4 factors that affect the absorption of drugs into the bloodstream: (1) Bioavailability: The amount (quantity %) that reaches the blood or plasma. Enzyme induction . e.e. 2. Parasympathetic vs.drug A induces the body to produce more of an enzyme which metabolises drug B. i. For example. However. pKa.Inhalation [i.e. steroids for asthma] . Hendersson-Hasselbach) Coated tabs (buffered) Gastric Emptying. via the co -administration of a receptor antagonist and an agonist for the same receptor. whereas for even a very toxic substance such as snake venom there is a dose for which there is no toxic effect detectable. some are inactivated by the liver before reaching systemic circulation. cocaine] . the subject of such study is the effect of an external substance or condition and its deleterious effects on living things: organisms. antibiotics. Toxicity can refer to the effect on a whole organism. antifungals] Key Concepts of Drug Activity 1. organ systems. Drug A effectiveness is not altered. the effects are increased or decreased. subcellular units. such as a human or a bacterium or a plant. individual organs. intramuscular. a drug’s major effect is produced by the amount of drug that is free in plasma. affects the activity of a drug. cells. thus an elevation of drug B occurs possibly leading to an overdose. Enzyme inhibition . as well as drugs & herbs (drug-herb interactions). Pharmacodynamics: the drug’s effect on the body. also increasing bioavailability. In the science of toxicology.g. another drug.
or magnesium. The curves are usually qualitative . with the steepest portion in the middle. such as emphysema. difficulty in urination due to an enlarged prostate gland -When using this product: avoid alcoholicbeverages -Ask a doctor or pharmacist before use if you are taking: sedatives or tranquilizers . they may be readily excreted at this point. since nicotine can increase your heart rate -Ask a doctor or pharmacist before use if you are: taking a prescription drug for depression or asthma (your dose may need adjustment). During these reactions. -Do not use: if you continue to smoke. mildly reduces blood pressure. high blood pressure. St John's wort. and involve the interactions of the polar functional groups of phase I metabolites. Garlic lowers total cholesterol levels. glutathione or amino acids ) — are usually detoxication in nature. be aware that the recommended dose of this product contains about as much caffeine as a cup of coffee -When using this product: increased dryness or irritation of the skin may occur immediate ly following use of this product or if you are using other topical acne drugs at the same time. ask a doctor or pharmacist before use if you are : taking theophylline(oral asthma drug). diabetes. glaucoma. difficulty in urination due to an enlarged prostate gland -When using this product: avoid alcoholicbeverages -Ask a doctor before taking if you: consume three or more alcohol-containing drinks per day. stomach pain.g. diabetes. Nigella sativa (Black cumin) is a general medicinal plant used for cough. thyroid disease. Central Nervous System [4 Qs] 2. or asthma -When using this product: alcohol. Examples of some commonly used herbal medicines: Artichoke and several other plants reduced total serum cholesterol levels. The stronger a particular substance is. it is the logarithm of the dose that is plotted on the X axis. Phase I metabolism usually precedes Phase II. or difficulty in urination due to an enlarged prostate gland -Ask a doctor before use if you: have high blood pressurenot controlled by medication.1. chew tobacco. the Y-axis usually is designated by percentages. micrograms . aspirin. irritability. breathing problems. many phase I products are not eliminated rapidly and undergo a subsequent reaction in which an endogenous substrate combines with the newly incorporated functional group to form a highly polar conjugate. ibuprofen. avoid alcoholic beverages -Ask a doctor or pharmacist before use if you are: taking sedatives or tranquilizers -Ask a doctor before use if you have: glaucoma or difficulty in urination due to an enlarged prostate gland -Ask a doctor before use if you: have heart disease. hypertension and stomach ache. magnesium salicylate . If the metabolites of phase I reactions are sufficiently polar. anxiety. and high blood pressure. have heart disease or have had a recent heart attack or irregular heartbeat. -Ask a doctor before use if you have: kidney disease and the laxative contains phosphates. a prescription drug for high blood pressure or depression -Ask a doctor before use if you have: glaucoma or difficulty in urination due to an enlarged prostate. or vomiting Antiemetics Nighttime Sleep Aids Antihistamines Pain Relievers Stimulants Antitussives (Cough Medicine) Bronchodilators Topical Acne Drugs Laxatives A dose-response curve is a simple X-Y graph relating the amount of a drug or toxin given to the response of the organism to that drug. asthma. Too much caffeine can cause nervousness. and anti -fungal herb. proving more effective than a placebo for the treatment of mild to moderate depression. the desired effects are found at doses slightly greater than the threshold dose. The seeds are considered carminative. Sedatives . Important to read the label of these products to learn about various drug interaction warnings for each ingredient. use snuff. Peppermint tea for problems with the digestive tract . pulmonary infections. such as emphysema or chronic bronchitis. and in such cases the curve is typically sigmoidal . thyroid disease. only one drug should be used unless directed by your doctor Category Acid Reducers ( H2 Receptor Antagonists) Antacids Sample Drug Interaction Information -For products containing cimetidine. influenza. or grams per kilogram of body-weight) is generally plotted on the X axis and the response is plotted on the Y axis. undesired side effects appear and grow stronger as the dose increases. though not necessarily.. glaucoma. reduction or hydrolysis reactions. Grapefruit seed extract as a natural antimicrobial has minimal effectiveness as an anti-bacterial.2. chronic bronchitis. including irritable bowel syndrome and nausea. sleeplessness. Psychotropics (antipsychotic & antidepressant ) 3 . which results in (more) polar metabolites of the original chemicals. Echinacea extracts limit the length of colds in some clinical trials.hypnotics & alcohols 2. or phenytoin (seizure drug) -Ask a doctor or pharmacist before use if you are: allergic to milk or milk products if the product contains more than 5 grams lactose in a maximum daily dose. Phase I reactions may occur by oxidation. and has antibacterial properties. diuretic and galactogogue. nausea. allergy.) -When using this product: limit the use of foods. when the 50% mark refers to LD50). though they can use quantitative information. reduces platelet aggregation.Category Nasal Decongestants Nicotine Replacement Products Sample Drug Interaction Information -Ask a doctor before use if you: have heart disease. If this occurs. with glucuronic acid. Seed powder or oil is externally applied for eruptions of skin. At higher doses still. beverages. used extensively in India for sleeplessness.3. or use othernicotinecontaining products -Ask a doctor or pharmacist before use if you are: taking sedatives or tranquilizers -Ask a doctor before use if you have: a breathing problem such as emphysema or chronic bronchitis. However. (The following ingredients are found in different OTC pain relievers: acetaminophen. polar bodies are either introduced or unmasked. -Ask a doctor before use if you have: kidney disease -Ask a doctor or pharmacist before use if you are: taking sedatives or tranquilizers -Ask a doctor before use if you have: a breathing problem. and occasional rapid heart beat. Black cohosh and other plants that contain phytoestrogens have some benefits for treatment of symptoms resulting from menopause. anti-parasitic. the steeper this curve will be. has yielded positive results.0. high blood pressure. In quantitative situations. and other drugs that have caffeine. sulfonates (commonly known as sulfation) . although some studies have found it to have no effect. The measured dose (usually in [[milligrams. Phase I and Phase II reactions are biotransformations of chemicals that occur during drug metabolism. Valerian root can be used to treat insomnia . The first point along the graph where a response above zero is reached is usually referred to as a threshold -dose. Anticonvulsants & anti-Parkinson 2.4. or difficulty in urination due to an enlarged prostate gland. Antianxiety & conscious sedation drugs 2. and tranquilizers may increase drowsiness. Phase II reactions — usually known as conjugation reactions (e. ketoprofen. which refer to the percentage of users registering a standard response (which is often death. For most beneficial or recreational drugs. stimulant. Rauvolfia Serpentina. potassium. and naproxen. sedatives. Commonly. 2. warfarin (blood thinning drug).
some get insomnia) olanzapine (Zyprexa®) Anti-depressants An antidepressant is a medication designed to treat or alleviate the symptoms of clinical depression. Many anticonvulsants block Sodium (Na+) channels . AMPA receptors or NMDA receptors . Venlafaxine Alaproclate . Smaller doses are generally used for this purpose. and they often take effect more quickly. relaxation. Sertraline Zimelidine . reduction of anxiety. including serotonin. Moclobemide Amineptine. Nefazodone. and post-herpetic neuralgia. Melitracen . Fluoxetine. Vanoxerine. Quaalude®) ethchlorvynol (Placidyl®) chloral hydrate (Noctec ®) meprobamate (Miltown ®) glutethimide ( Doriden ®) methyprylon (Noludar ®) gamma-hydroxybutyrate (GHB) ethyl alcohol (alcoholic beverage) diethyl ether (Ether) methyl trichloride (Chloroform) zopiclone (Imovane®. Sedatives may be referred to as tranquilizers. Tricyclic antidepressants (TCAs ) prevent the reuptake of various neurotransmitters . Tranylcypromine Brofaromine. Monoamine oxidase inhibitors (MAOI) Harmaline. There are currently two main types: 1. Trazodone Mirtazapine Reversibleinhibitor of monoamineoxidase A (RIMA) Dopamine reuptake inhibitor(DARI) Norepinephrine-dopamine reuptake inhibitors Norepinephrine reuptake inhibitor(NRI) or (NARI) Serotonin -norepinephrine reuptake inhibitor (SNRI) Selective serotonin reuptake inhibitor(SSRI) Selective serotonin reuptake enhancer (SSRE) Tricyclicantidepressants (TCA) Tetracyclic antidepressants Noradrenergic and specific serotonergic antidepressant (NaSSA) 4 . Many antidepressants also are used for the treatment of anxiety disorders . poor judgment. Modafinil Bupropion Atomoxetine. notably the tricyclics . Tianeptine Amitriptyline Amoxapine. norepinephrine. schizophrenia.g. Nortriptyline. The word neuroleptic is derieved from Greek. whereas earlier monoamine oxidase inhibitors (MAOIs) blocked the destruction of neurotransmitters by enzymes which normally break them down. Viloxazine Duloxetine. Trifluoperaz®) loxapine succinate (Loxitane®) perphenazine (Etrafon®. These drugs include: Barbiturates Benzodiazepines Zolpidem Zaleplon Zopiclone Eszopiclone chloral hydrate Chlormethiazole Antihistamines Doxylamine Promethazine diphenhydramine. Antipsychotics are also referred to as neuroleptic drugs. A physician will usually recommend alternative sleeping patterns and exercise before prescribing medication for sleep. Selegiline. downers. Typical antipsychotics ("major tranquilizers") fluphenazine (Prolixin®) haloperidol (Haldol ®) thiothixene (Navane®) trifluoperazine (Stelazine®. The main classes of antidepressants have similar efficacy. Anti-Convulsants 1 Aldehydes 2 Aromatic allylic alcohols 3 Barbiturates 4 Benzodiazepines 5 Bromides 6 Carbamates 7 Carboxamides 8 Fatty acids 9 Fructose derivatives 10 Gaba analogs 11 Hydantoins 12 Oxazolidinediones 13 Propionates 14 Pyrimidinediones 15 Pyrrolidines 16 Succinimides 17 Sulfonamides 18 Triazines 19 Ureas 20 Valproylamides (amide derivatives of valproate) Antipsychotics are drugs used to treat psychosis (e. myofascial pain syndrome. sleepiness. Escitalopram. Butriptyline. belong to a diverse group of pharmaceuticals used in prevention of the occurrence of epileptic seizures. The anticonvulsants. However. no such drug exists. SSRI’s specifically prevent the reuptake of serotonin (thereby increasing the level of serotonin in synapses of the brain). Phenmetrazine. Some anticonvulsants inhibit the metabolism of GABA or increase its release. Calcium (Ca2+) channels. Reboxetine. Etoperidone. resulting in calmness. Nialamide. Mechanism of action: The therapeutic effects of antidepressants are believed to be related to an effect on neurotransmitters . Desipramine. slurred speech. Some antidepressants. mania and delusional disorder. Examples of sedatives Antidepressants mirtazapine (Remeron®) trazodone (Desyrel®) Barbiturates secobarbital (Seconal®) pentobarbital (Nembutal ®) amobarbital (Amytal ®) Benzodiazepines ("minor tranquilizers") alprazolam (Xanax®) diazepam (Valium®) lorazepam (Atavan ®) Herbal sedatives catnip Valerian (plant) Mandrake Kava Kava Uncategorized sedatives eszopiclone (Lunesta®) ramelteon (Rozerem®) methaqualone (Sopor®. Toloxatone. Imipramine. Antipsychotics also have some effects as mood stabilizers . Trilafon®) prochlorperazine (Compazine®) 2. staggering gait . Protriptyline. Doxepin . many of these drugs can cause unconsciousness (see hypnotic) and death. Opipramol . and dopamine. Alcohol is often tried as a hypnotic drug but it is not particularly effective. and slow. particularly by inhibiting the monoamine transporter proteins of serotonin and norepinephrine. however. whether or not the patient is depressed. Fluvoxamine. Zimovane ®) chloral hydrate (Noctec ®) zaleplon (Sonata ®) zolpidem (Ambien®) Hypnotic drugs are a class of drugs that induce sleep (which differentiates them from the sedative category). Paroxetine. Citalopram. and tricyclic antidepressants are used in the treatment of chronic pain disorders such as chronic functional abdominal pain (CFAP). . Mianserin . but the newer types are generally regarded to have a more benign side -effect profile and less risk of lethality if taken in overdose. soporifics. . Maprotiline. Milnacipran . leading to their frequent use in treating mood disorder (particularly bipolar disorder) even when no signs of psychosis are present. Clomipramine. anxiolytics. or sedative-hypnotics. 'Neuro ' refers to the nerves and 'lept' means 'to take hold of'. Thus the word means 'taking hold of one's nerves' which implies their role in mood stabilization. Dothiepin . Atypical antipsychotics clozapine (Clozaril®) quetiapine (Seroquel®) risperidone (Risperdal ®) ziprasidone (Geodon®) (some become tired. depressants. Often the treatment of insomnia will not begin with drugs at all.A sedative is a substance that depresses the central nervous system (CNS). Isocarboxazid . as many (not all) hypnotic drugs are habit forming. a good anticonvulsant would prevent the spread of the seizure within the brain and offer protection against possible excitotoxic effects that may result in brain damage. sleeping pills. are commonly used off-label in the treatment of neuropathic pain. The goal of an anticonvulsant is to suppress the rapid and excessive firing of neurons that start a seizure. Lofepramine. At high doses or when they are abused. Failing this. Phenelzine. used in the treatment of severe insomnia and in surgical anesthesia. Trimipramine Maprotiline. slowed breathing. Iproclozide Iproniazid . An excellent anticonvulsant would have few serious side effects. uncertain reflexes. sometimes also called antiepileptics. Dibenzepin . Iprindole.
a type of prostatitis. cholinergic. The parasympathetic nervous system is entirely cholinergic.Salmeterol Tamsulosine . on ß-adrenergic receptors . the peripheral nervous system. Indications for beta blockers include: Hypertension Angina Cardiac arrhythmia Congestive heart failure Myocardial infarction Glaucoma Migraine prophylaxis Symptomatic control (tachycardia . A substance is cholinergic if it is capable of producing. and the binding of an agonist will generally cause the cell to respond in a fight-or-flight manner. tremor) in anxiety and hyperthyroidism Essential tremor Phaeochromocytoma. also known as a cholinergic agent or a parasympathomimetic . A cholinergic. As a side effect they may reduce blood pressure and result in lightheadedness. which are a class of G protein-coupled receptors that are targets of the catecholamines. Examples of alpha blockers: Alpha blockers include: •Doxazosin (Cardura) •Prazosin (Minipress ) •Phenoxybenzamine •Phentolamine (Rogitine) •Tamsulosin (Flomaxtra/Flomax) •Alfuzosin (Uroxatral) •Terazosin (Hytrin) Beta blockers are a class of drugs used for various indications. ----------------------------An anticholinergic agent is a member of a class of pharmaceutical compounds which serve to reduce the effects mediated by acetylcholine in the central nervous system and peripheral nervous system. lung.Piruterol . or both. in conjunction with a-blocker 5 .Methoxamine Norepinephrine . and are classified according to the receptors that are affected: antimuscarinic agents operate on the muscarinic acetylcholine receptors . as well as cholinergic enzymes such as the anticholinesterases.Metaproterenol . and blood flow diverted from other organs to skeletal muscle. the catecholamines adrenaline and noradrenaline (also called epinephrine and norepinephrine in the USA). energy will be mobilized. Cholinergics 3. Adrenergics 3. Indications: These drugs may be used to treat: •benign prostatic hyperplasia (BPH) •high blood pressure (hypertension). ß1-Adrenergic receptors are located mainly in the heart. acetylcholine receptor agonists (such as muscarine and nicotine). is any chemical which functions to enhance the effects mediated by acetylcholine in the central nervous system. and adipose tissue. This is not typically the drug of choice unless the patient also has BPH. Direct Acting: Albuterol – Clonidine – Dobutamine – Dopamine . The role and location of ß3-receptors is less well-defined. but particularly for the management of cardiac arrhythmias and cardioprotection after myocardial infarction. The majority of anticholinergics are antimuscarinics . or releasing acetylcholine. Beta blockers block the action of endogenous catecholamines. GI tract. Blocking agents (adrenergic. •symptoms of non inflammatory chronic pelvic pain syndrome. altering. etc) Adrenergic Agents bind with adrenergic receptors (or adrenoceptors). Anticholinergics are typically reversible competitive inhibitors of one of the two types of acetylcholine receptors .Formoterol . Many cells possess these receptors. ß2 and ß3. ß2-Adrenergic receptors are located mainly in the heart.Isoproterenol . There are three known types of beta receptor. part of the sympathetic nervous system which mediates the "fight or flight" response. designated ß1. liver. For instance.3.3. and antinicotinic agents operate on the nicotinic acetylcholine receptors .Phenylephrine .2. Anticholinergic Drugs Unclassified benztropine (Cogentin®)` Nicotinic receptor antagonists Ganglionic blocking agents Nondepolarizing neuromuscular blocking agents Trimethaphan Muscarinic receptor antagonists Belladonna alkaloids Scopolamine (L-Hyoscine) Atropine (D/L-Hyoscyamine) Synthetic and Semisynthetic Dicyclomine Flavoxate Ipratropium Oxybutynin Pirenzepine Tiotropium Tolterodine (Detrusitol®) Tropicamide Solifenacin (Vesicare®) Darifenacin (Enablex®) Depolarizing neuromuscular blocking agents Atracurium Doxacurium Mivacurium Pancuronium Tubocurarine Vecuronium Suxamethonium chloride Alpha blockers (also called alpha-adrenergic blocking agents) constitute a variety of drugs which block a1 -adrenergic receptors in arteries and smooth muscles. Adrenergic receptors specifically bind their endogenous ligands . kidney.Epinepherine . These include acetylcholine's precursors and cofactors . epinephrine (adrenaline) and norepinephrine (noradrenaline) in particular. Autonomic [3 Qs] 3. and are activated by these. the heart rate will increase and the pupils will dilate.Tamsulosine – Terbutaline Amphetamine – Tyramine Ephedrine Indirect Acting Mixed Action: A synapse is cholinergic if it uses acetylcholine as its neurotransmitter. pancreas.0.1. Cholinergic means "related to the neurotransmitter acetylcholine". and skeletal muscle.
g. decreasing afterload. antiarrhythmic agents are often still in use to suppress arrhythmias. Digoxin is widely used in the treatment of various heart conditions. Moricizine.1 Adrenergic neuron blockers 1. Some of these compounds (ouabain and some frog poisons) are used in Africa as arrow-poisons for hunting. amlodipine. reducing heart rate & improving coronary blood flow. Cardiac output is restored but atrial fibrillation or atrial flutter are not abolished. These drugs are Calcium ion antagonists and are used for treatment of exertional & vasospastic angina. and ventricular fibrillation. Digoxin Antihypertensives: 1. reducing the number of impulses reaching the ventricles. Prajmaline. improving myocardial efficiency.4. Suppression is often done to relieve the symptoms that may be associated with the loss of the atrial component to ventricular filling (atrial kick ) that is due to atrial fibrillation or flutter. Dofetilide. such as atrial fibrillation. nitrates such as nitroglycerin (glyceryl trinitrate) or pentaerythritol tetranitrate These drugs cause vasodilation of the venous capacitance vessels by simulating the endothelium-derived relaxing factor (EDRF). ---------------------3. Cardiac glycosides work by inhibiting the Na+/K+ pump. Drugs used are: 1.3. This inhibition increases the amount of Ca++ ions available for contraction of the heart muscle. beta blockers . Diuretics: help the kidneys eliminate excess salt and water from the body's tissues and blood. epitizide.6 Aldosterone antagonists 1. Cardiovascular [4 Qs] 4. In individuals with ventricular arrhythmias. improves cardiac output and reduces distention of the heart. and reduces the likelihood of dementia. Anti-anginal agents 4. atrial flutter. Class II agents are anti-sympathetic nervous system agents (all: beta blockers ).4 ACE inhibitors 1. namely atrial fibrillation. digitoxin ---------------------------------------------------------------. digitalis.3 Calcium channel blockers 1. Evidenc e suggests that reduction of the blood pressure by 5-6 mmHg can decrease the risk of stroke by 40%.Strophanthus .) Anti-anginal agents: for treatment of angina pectoris. either Class I agents (e.-------------------------------------------class Ia:Ajmaline . hydrochlorothiazide & chlorothiazide) -Thiazide-like diuretics: (indapamide. Sparteine class Ib: Aprindine. T hey have negative inotropic & chronotropic effects. torsemide) -Thiazides: (chlortalidone. but also in some animals. Antiarrhythmic agents are used to suppress fast rhythms of the heart (cardiac arrhythmias). of coronary heart disease by 15-20%.1. Lidocaine . Class II agents (e.g.---------------------------------------Digoxin is a cardiac glycoside extracted from the foxglove plant.ouabain g/k/e-strophanthin . Procainamide.digoxin. Its corresponding aglycone is digoxigenin.Digitalis lanata and Digitalis purpurea ..2 Anti-adrenergics 1.9 Herbals provoking hypotension 1. atrial flutter and congestive heart failure that cannot be controlled by other medication. Bretylium tosilate. furosemide. Tocainide class Ic:Encainide. reducing the pressure in the ventricles and so reducing wall tension and oxygen requirements in the heart. T hey have an antiarrhythmic effect by prolonging the refractory period of the AV node (Atrioventricular node). They do this by stabilizing the E2-P transition state of the Na+/K+ pump. or the Class III agent diltiazem. calcium channel blockers . Bunaftine. Class V agents work by other or unknown mechanisms. metolazone) -Potassium-sparing diuretics : (amiloride.diuretics 4. Digoxin preparations are commonly marketed under the trade name Lanoxin. Mexiletine. ---------------------------------------------------------------. ventricular tachycardia. either cardioselectives such as acebutolol or metoprolol . 6 . and mortality from cardiovascular disease. Examples of plants producing cardiac glycosides: .5 Angiotensin II receptor antagonists 1.5. Antiarrhythmics 4. Disopyramide.7 Vasodilators 1. Class IV agents affect the AV node. These glycosides are found as secondary metabolites in several plants.. Anticoagulants. Class III agents affect potassium (K+) efflux. In vitro.Beta-Blocking Drugs Non-selective agents Alprenolol Carteolol Levobunolol Mepindolol Metipranolol Nadolol Oxprenolol Penbutolol Pindolol Propranolol Sotalol Timolol ß1-Selective agents Acebutolol Atenolol Betaxolol Bisoprolol Esmolol Metoprolol Nebivolol Mixed a1/ß-adrenergic antagonists Carvedilol Celiprolol Labetalol ß2-Selective agents Butoxamine (weak a-adrenergic agonist activity) 4. a symptom of ischaemic heart disease.1 Diuretics 1. Propafenone class II: various Beta blockers class III:Amiodarone. nifedipine). Antihypertensives . Lorcainide.8 Centrally acting adrenergic drugs 1.2. Quinidine.0. They cannot be used in vasospastic angina and can precipitate heart failure. Flecainide. verapamil). ethacrynic acid. Used to relieve both exertional and vasospastic angina by allowing venous pooling. There are several types including: -Loop diuretics: (bumetanide.8. triamterene) (NOTE: evidence suggest that by lowering blood pressure. Ibutilide class IV: various Calcium channel blockers class V:Adenosine. ---------------------------------------------------------------. Short-acting nitrates are used to abort angina attacks that have occurred. coagulants & antihyperlipidemics Cardiac glycosides are drugs used in the treatment of congestive heart failure and cardiac arrhythmia. --------------------2. If these drugs fail it may lead to implantation of an implantable cardioverter-defibrillator (ICD). they dilate coronary & peripheral arteries. Cardiac glycosides 4. or noncardioselectives such as oxprenolol or sotalol These drugs are used in the prophylaxis of exertional angina by reducing the work the heart is allowed to perform below the level that would provo ke an angina attack.-------------------------------------------5 main classes in the Vaughan Williams system of antiarrhythmic agents: Class I agents interfere with the sodium (Na+) channel. heart failure. while longer-acting nitrates are used in the prophylactic management of the condition.
This decreases LDL by 15-30% and raises HDL by 3-5%. Phenindione. The activated platelets then release the contents of their granules. Thrombin ineffective with these agents because of inactivation as a result of pH factors. Hirudin. Can be cut or shaped. Dermatan sulfate. used understents. More expensive thanGelfoam . Surgicel. Not available in the United States at this time. Swells upon contact with blood. "the good cholesterol". This is useful in primary and secondary prevention of deep vein thrombosis . Phenprocoumon. lepirudin. Iloprost. Melagatran. Enoxaparin. Ancrod. Fibrinolysin. Helistat Thrombin ineffective with these agents due to inactivation as a result of pH factors. 5. Heparin. Works as a competitive inhibitor of plasminogen activation. Fibrin/tissue glue. 6. Picotamide. Anistreplase. Dabigatran.I. pulmonary embolism. For severebleeding. they are most effective when consumed with meals. Risk with resins is G. 4. Cote 3 / in× 1. coagulation from a cut on the skin is not initiated by air or drying out. Diphenadione. Exerts physical effect rather than physiologic. Desirudin. and may also cause liver damage. Clorindione. bile acid sequestrants (resins) are particularly effective for lowering LDL -C by sequestering the cholesterol-containing bile acids released into the gut and preventing their reabsorption. but does not stick to instruments. Instat Absorbable collagen made from purified and lyophilized bovine dermal collagen. Contrary to popular belief. gloves. Oxycel After 24-48 h.1. Treprostinil. Vasoconstrictors 7 . MCH attracts platelets and triggers aggregation in fibrous mass. In cases when an immediate effect is required. dentures. All are superior 4 hemostats for moderate-to -severebleeding. Risk of severe muscle damage (myopathy & rhabdomyolysis) with fibrates. 1. Moderate-t -severe o bleeding. The studies show they lower LDL-C by 18% to 55%. It has little effect on triglycerides. Protein C. these contain a variety of substances that stimulate further platelet activation and enhance the haemostatic process. heparin must be given concomitantly. Fibrates may decrease LDL. Can be sutured into place. Anticoagulants are given to people to stop thrombosis (blood clotting inappropriately in the blood vessels). is also well-suited for lowering triglycerides by 2050%. 2. that is. Shaped according to intended use. Oxidized regenerated cellulose. One5000 -unit vial dissolved in 5mL of saline solution can clot equal amount of blood in less than 1 sec. fibrous. Clopidogrel. Indobufen. phytosterols reduce the absorption of cholesterol in the gut. Helpful to place topical Thrombin onGelfoam . Some lower lower bad cholesterol (low density lipoproteins) and others may increase high density lipoprotein (HDL). Useful in short term (2 d) for preventing hemorrhage -8 following dental extractions. anti-hyperlipidemics ). nicotinic acid. Warfarin Antithrombin III. Local anesthetics [4 Qs] 5. EDTA . Dry. Level of the good cholesterol HDL i s also increased. it becomes gelatinous. Fully resorbed in 10 -14 days. Thrombogen Cyklokapron Beriplast There are several classes of hypolipidemic drugs (a. Parnaparin . statins are good at lowering LDL. Ximelagatran Dabigatran. Ticlopidine. Nadroparin. Disorders in coagulation can lead to increased hemorrhage and/or thrombosis and embolism. coagulation is initiated within 20 seconds after an injury occurs to the blood vessel damaging the endothelial cells. 3. It is important to note that they take at least 48 to 72 hours for the anticoagulant effect to develop fully. Plug 3/8 in× 3/ in. Epoprostenol . Bemiparin . Fondaparinux.k. but by platelets adhering to and activated by collagen in the blood vessel endothelium. Absorbable dressings from bovine collagen. and bivalirudin. Dicumarol (Dicoumarol}. which is strongly linked to cardiovascular diseases. fibrates are indicated for hypertriglyceridemia . Hence. Tenecteplase. Tinzaparin Abciximab. 1. Saruplase . which blocks thrombin from clotting blood. Drotrecogin alfa. Tirofiban. Danaparoid.5 in. Acetylsalicylic acid (Aspirin). Many different hemostatic agents!!!! (need table) Product Gelfoam Description Absorbable gelatin sponge made from purified gelatin solution. Eptifibatide. Nicotinic acid may cause hyperglycemia. Used as a rinse. HCl acid salt purified bovine corium collagen. Thrombinar . 2. Basic pharmacology 5. Ethyl biscoumacetate. 4 Tape 1 in× 3 in. Prasugrel . Absorbs in 3 -5 days. Defibrotide. Colla-Cote. Beraprost. Urokinase Argatroban.Vitamin K antagonists: An anticoagulant is a substance that prevents coagulation. Derived from bovine sources. Rivaroxaban Citrate. with resulting pressure adding tohemostasis. Directly converts fibrinogen to fibrin.2.0. Carbasalate calcium.. This is called primary haemostasis . For extensive or invasive surgery. sterile. Plug Thrombostat. Sulodexide. Can be left in place or removed. Brinase. Risk of severe muscle damage (myopathy & rhabdomyolysis) with statins. In a normal individual. ezetimibe (Zetia) is a selective inhibitor of dietary cholesterol absorption. and may also reduce the absorption of other drugs and vitamins from the gut. though generally less than statins. Direct thrombin inhibitors: Another type of anticoagulant is the direct thrombin inhibitors . or gauze sponges. like fibrates . Similar to ezetimibe. Bivalirudin. Reviparin. or alone. it stops blood from clotting. Platelets immediately form a haemostatic plug at the site of injury. It works by activating antithrombin III. It may also lower LDL by 5-25% and increase HDL by 15-35%. water insoluble. oneshould consider placing inside a splint. Tranexamic acid. Secondary haemostasis then follows —plasma components called coagulation factors respond (in a complex cascade) to form fibrin strands which strengthen the platelet plug. 5. Dipyridamole. Vitamin K antagonists: Oral anticoagulants are a class of pharmaceuticals that act by antagonizing the effects of vitamin K. Topical thrombin. Heparin group (Platelet aggregation inhibitors): Acenocoumarol. Dalteparin. Triflusal Alteplase. Heparin and derivative substances: Heparin is a biological substance. Tioclomarol. myocardial infarctions and strokes in those who are predisposed. Fibrates typically lower triglycerides by 20% to 50%. It is an important part of hemostasis (the cessation of blood loss from a damaged vessel) whereby a damaged blood vessel wall is covered by a fibrin clot to stop hemorrhage and aid repair of the damaged vessel. The most important oral anticoagulants are Warfarin (Coumadin). Microfibrillar collagen hemostat (MCH). problems. Useful to control bleeding when other agents ineffective. Avitene. depending on the specific statin being used. Adheres to bleeding surfaces when wet. Ditazole.a. Cloricromen. Streptokinase. Mild -to -moderate bleeding is usually controlled in 2 -5 min. Tape. Oxalate Other platelet aggregation inhibitors: Enzymes: Direct thrombin inhibitors: Other antithrombotics: Non-medicinal: The coagulation of blood is a complex process during which blood forms solid clots. Aloxiprin. usually made from pig intestines. Reteplase. Indications and features Useful for most patients taking anantithrombotic agent. Lepirudin. phytosterols may be found naturally in plants. Current members of this class include argatroban.
Antibiotics can also be classified by the organisms against which they are effec tive. Antineoplastics Antibiotics Antibiotics Antibiotics Antibiotics Antibiotics An antibiotic is a drug that kills or slows the growth of bacteria . such as vasopressin receptors or adrenoreceptors . The effectiveness of individual antibiotics varies with the location of the infection.4. Adverse reactions to local anesthetics are not infrequent. which are often added as preservatives to local anesthetic solutions. Vasoconstriction also occurs in superficial blood vessels of warm -blooded animals when their ambient environment is cold. this process diverts the flow of heated blood to the center of the animal. Some antibiotics have been derived from mold. for example the penicillin class. such as Gramnegative or Gram-positive bacteria. --------------------------Methemoglobinemia: The systemic toxicity of prilocaine is comparatively low. this side effect is potentially life-threatening. Vasoconstrictors are also used clinically to increase blood pressure or to reduce local blood flow. Prilocaine is not recommended for use in infants. such as Escherichia coli and Klebsiella Hearing loss Vertigo Kidney damage Common Uses Side Effects 8 . Antifungals 6. They are not enzymes. vasodilation.3. also vasopressor and simply pressor . Local anesthetic drugs act mainly by inhibiting Levobupivacaine sodium influx through sodium-specific ion Lidocaine channels in the neuronal cell membrane. skin tests and provocative challenge may be necessary to establish a diagnosis of allergy. fungi. Acidosis such as caused by wound infection partly reduces the action of local anesthetics because of reduced ability to cross the cell membrane. Vasoconstrictors Antihistamines Adrenaline Asymmetric dimethylarginine ATP Cannabis Catecholamines Cocaine Decongestants Endothelin Phenylephrine Pseudoephedrine Neuropeptide Y Norepinephrine Tetrahydrozoline hydrochloride Thromboxane 6.A local anesthetic is a drug that reversibly inhibits the propagation of signals along nerves. effects such as analgesia (loss of Benzocaine pain sensation) and paralysis (loss of muscle Chloroprocaine power) can be achieved. but true allergyis very rare.0. Some antibiotics actually kill the bacteria (bactericidal). is known to cause methemoglobinemia. There are also cases of allergy to paraben derivatives. Antibiotics are generally small molecules with a molecular weight less than 2000 kd. which depends on the sensitivities of the organisms that most commonly cause the infection and the concentration of antibiotic obtainable in the affected tissue. A vasoconstrictor . Local anesthetics are weak bases and are usually formulated as the Combinations Lidocaine/prilocaine (EMLA) hydrochloride salt to render them watersoluble. and by the type of infection in which they are useful. Prilocaine When the influx of sodium is interrupted. is any substance or that acts to cause vasoconstriction (narrowing of the lumena of blood vessels) and usually results in an increase of the blood pressure. These so-called synthetic local Bupivacaine anesthetics are structurally related to cocaine . The opposite process. Non-allergic reactions may resemble allergy in their manifestations. the ability of the antibiotic to reach the site of infection. In some cases. is the opening of blood vessels. As methemoglobinemiareduces the amount of hemoglobin that is available for oxygen transport. and the ability of the bacteria to resist or inactiva te the antibiotic. in Mepivacaine particular the voltage-gated sodium channels. Many vasoconstrictors act on specific receptors. They have no effect against viruses.2. Antibacterials 6. Class Aminoglycosides Generic Name Amikacin Gentamicin Kanamycin Neomycin Netilmicin Streptomycin Tobramycin Carbacephem Carbapenems Loracarbef Ertapenem Imipenem/ Cilastatin Meropenem Primaxin Nebcin Lorabid Brand Names Amikin Garamycin Infections caused by Gram-negative bacteria. Chemotherapy [5 Qs] 6. an Ropivacaine action potential cannot arise and signal Septocaine conduction is inhibited. whereas others merely prevent the bacteria from multiplying (bacteriostatic ). Antivirals 6. When it is used on specific nerve Amino esters pathways. Clinical local Cocaine anesthetics belong to one of two classes: Procaine aminoamide and aminoester local Amino amides anesthetics. Therefore dose limits for prilocaine should be strictly observed. or parasites. Exposure to moderately high levels of stress also induces vasoconstriction. however its metabolite. Antibiotics can be categorized based on their target specificity: 'narrowspectrum' antibiotics target particular types of bacteria. preventing the loss of heat.1. while 'wide -spectrum' antibiotics affect a larger range of bacteria. o-toluidine.
chlamydial infections. usually applied directly to the eye or inhaled into the lungs. syphilis. mycoplasmal infections. gonorrhea Common Uses Side Effects Polypeptides Colistin Polymyxin B Ciprofloxacin Ciproxin. Lyme disease. and diarrhea (especially at higherdoses) Jaundice Cefzil Ceftin Brand Names Duricef Ancef Keflex Ceclor Mandole Gastrointestinal upset and diarrhea Nausea (if alcohol taken concurrently) Allergic reactions Vancomycin Macrolides Azithromycin Clarithromycin Vancocin Zithromax . bacterial prostatitis. Ciplox Brand Names Mupirocin Common Uses Eye. vomiting. rarely given by injection Side Effects Kidney and nerve damage (when given by injection) Nausea (rare) Antibiotics Antibiotics Antibiotics Antibiotics Antibiotics Class Sulfonamides Generic Name Mafenide Prontosil (archaic) Sulfacetamide Sulfamethizole Sulfanilimide (archaic) Sulfasalazine Sulfisoxazole Trimethoprim TrimethoprimSulfamethoxazole (Co-trimoxazole ) Tetracyclines Demeclocycline Doxycycline Minocycline Oxytetracycline Tetracycline Sumycin Vibramycin Syphilis. bacterial diarrhea. syphilis. acne rickettsial infections Bactrim Urinary tract infections (except sulfacetamide and mafenide). mycoplasmal infections . penicillin used for streptococcal infections.Antibiotics Antibiotics Antibiotics Antibiotics Antibiotics Class Cephalosporins (First generation ) Generic Name Cefadroxil Cefazolin Cephalexin Cephalosporins (Secondgeneration ) Cefaclor Cefamandole Cefoxitin Cefprozil Cefuroxime Cephalosporins (Third generation ) Cefixime Cefdinir Cefditoren Cefoperazone Cefotaxime Cefpodoxime Ceftazidime Ceftibuten Ceftizoxime Ceftriaxone Cephalosporins (Fourthgeneration) Cefepime Rocephin Maxipime Gastrointestinal upset and diarrhea Nausea (if alcohol taken concurrently) Allergic reactions Monobactam Aztreonam Fortum Troleandomycin Cefobid Claforan Gastrointestinal upset and diarrhea Nausea (if alcohol taken concurrently) Allergic reactions Erythromycin Omnicef Dirithromycin Streptococcal infections. Lymedisease Nausea. mafenide is used topically for burns Nausea. ear or bladder infections. Sumamed Biaxin Antibiotics Antibiotics Antibiotics Antibiotics Antibiotics Common Uses Side Effects Gastrointestinal upset and diarrhea Nausea (if alcohol taken concurrently) Allergic reactions Class Glycopeptides Generic Name Teicoplanin Brand Names Common Uses Side Effects Roxithromycin Antibiotics Antibiotics Antibiotics Antibiotics Antibiotics Antibiotics Antibiotics Antibiotics Antibiotics Antibiotics Brand Names Novamox Quinolones Gastrointestinal upset and diarrhea Allergy with serious anaphylactic reactions Brain and kidney damage (rare) Class Generic Name Bacitracin Class Generic Name Amoxicillin Ampicillin Azlocillin Carbenicillin Cloxacillin Dicloxacillin Penicillins Flucloxacillin Mezlocillin Nafcillin Penicillin Piperacillin Ticarcillin Trovafloxacin Trovan Wide range of infections. and Lyme disease Enoxacin Gatifloxacin Levofloxacin Lomefloxacin Moxifloxacin Norfloxacin Ofloxacin Ocuflox Avelox Tequin Levaquin Urinary tract infections. respiratory infections . and diarrhea Allergy (including skin rashes) Crystals in urine Kidney failure Decrease in white blood cell count Sensitivity to sunlight Brand Names Common Uses Side Effects Class Others Antibiotics Antibiotics Antibiotics Antibiotics Antibiotics Generic Name Chloramphenicol Clindamycin Ethambutol Fosfomycin Furazolidone Isoniazid Linezolid Metronidazole Nitrofurantoin Platensimycin Pyrazinamide Zyvox Flagyl Macrodantin Brand Names Chloromycetin Cleocin Common Uses Side Effects Gastrointestinal upset Sensitivity to sunlight Staining of teeth Potential toxicity to mother and fetus during pregnancy Quinupristin/ Dalfopristin Rifampin Spectinomycin Syncercide 9 . vomiting.
Foscarnet. Valrubicin). Gemtuzumab. Altretamine. Sulconazole. Podophyllum: ( Etoposide. Ganciclovir. BBR3464). Amsacrine. Trastuzumab Aminolevulinic acid. Celecoxib. Procarbazine. Vincristine. Evolutionary theory of genetic selection requires that as close as possible to 100% of the infecting organisms be killed off to avoid selection of resistance. the rate of antibiotic resistance is so high that the normal. Gemcitabine Taxane: ( Docetaxel. such as hospitals and some child-care locations. Pentostatin. low cost antibiotics are virtually useless for treatment of frequently seen infections. Inosine. making it possible for bacteria never exposed to an an tibiotic to acquire resistance from those which have. it has certainly done much to advance the state of antiviral technology. major advances in the techniques for finding new drugs. The situation is worsened by the fact that genes coding for antibiotic resistance can be transferred between bacteria. Cetuximab. Indinavir. probably via the enzyme 1. Mercaptopurine. 3. both fungi and humans are eukaryotes. Modes of action: antineoplastics work by inhibiting topoisomerase II which stops DNA being unwound. and the hepatitis B and C viruses. Econazole. the cause of the deadly acquired immunodeficiency syndrome ( AIDS) epidemic. Clofarabine. Delavirdine. Lomustine. Anagrelide. Pemetrexed. Others: Flucytosine is an antimetabolite. Alemtuzumab. Didanosine. the average susceptibility of this new population to the compound will be much less than that of the original population. Uramustine Folic acid: ( Methotrexate. Ribavirin. Idoxuridine. Purine: ( Cladribine. Caspofungin . Panitumumab. Hydroxyurea. ThioTEPA. Teniposide). Porfimer sodium. Lamivudine. Stavudine. Denileukin diftitox. Valaciclovir. Animal cells have cholesterol instead of ergosterol and are less susceptible: Nystatin . Imiquimod. Fotemustine. Melphalan). Tiaconazole. or "cytotoxic antibiotics". Paclitaxel). Oxiconazole . Vinca: ( Vinblastine .Interferon. By 1984 half of the people with active tuberculosis in the United States had a strain that resisted at least one antibiotic. Mechlorethamine. Pegaspargase . Vindesine. Micafungin 5. Arsenic trioxide. Clotrimazole . Fludarabine. Nevirapine Amprenavir. Fomivirsen. Epirubicin. Mitoxantrone. Butenafine. which is best known for causing cold sores but actually covers a wide range of diseases. Penciclovir. al lowing biomedical researchers to understand the structure and function of viruses. Fomivirsen. Mitotane. Zidovudine Antiviral drugs are a class of medication used specifically for treating viral infections. Naftifine . Ketoconazole. Pyrimidine: ( Capecitabine). Vidarabine Amantadine. Famciclovir. Bexarotene. Classes include: 1. This enzyme converts lanosterol to ergosterol. Dasatinib. Gefitinib. Itraconazole. which can cause liver cancer. Bevacizumab. Hydroxycarbamide. Platinum: ( Carboplatin. Temozolomide. Darunavir. Though no one could sensibly claim that AIDS has been a benefit to humankind. Researchers are now worki ng to extend the range of antivirals to other families of pathogens. Atazanavir. Irinotecan. Tioguanine). Bortezomib. Sertaconazole. see also neoplastics) are drugs that inhibit and combat the development of tumors. Cyclophosphamide. Mitomycin Topotecan. principally ergosterol and this causes the cell's contents to leak out and the cell di es. Erlotinib. and is required in fungal cell wall synthesis and block steroid synthesis in humans. An abscess caused by methicillin-resistant Staphylococcus aureus bacteria (MRSA).Use or misuse of antibiotics may result in the development of antibiotic resistance by the infecting organisms. Voriconazole. Dacarbazine. Mebendazole. Fosamprenavir. Lopinavir. Verteporfin Alitretinoin. Viramidine PIs Fusion inhibitors Other antiviral agents Chemotherapeutic agents/Antineoplastic agents Antineoplastics (or "antitumor antibiotics". Cisplatin. Filipin. This means it is more difficult to find a target for an antifungal medication to attack that does not also exist in the infected organism. Busulfan. Idarubicin. dactinomycin anthracyclines doxorubicin daunorubicin epirubicin which also inhibit topoisomerase II) other cytotoxic antibiotics Bleomycin. Fluorouracil. Podophyllotoxin. Most of the antivirals now available are designed to help deal with HIV. Isoconazole. Amorolfine. Fluocinonide. Anti-influenza agents NRTIs NtRTIs Antiretroviral drugs Tenofovir NNRTIs Efavirenz. Pimaricin. Zalcitabine. Cytarabine. Gentian Violet Anti-herpesvirus agents Aciclovir. Echinocandin: inhibit the synthesis of glucan in the cell wall. some of the side-effects of systemic anti fungals can be life -threatening. Rimocidin. 2. Natamycin . Thiabendazole. Examples actinomycin. Rituximab. Methyl aminolevulinate. Streptozocin). Oxaliplatin. Vinorelbine). Allylamines: inhibit enzyme squalene epoxidase. Tromantadine. which is required for both DNA replication and RNA/protein synthesis. Imatinib. since they have descended from those few organisms which survived the original treatment. Chlormethine. Asparaginase . an enzyme required for ergosterol synthesis: Terbinafine (Lamisil ). Nitrosoureas: ( Carmustine. Rimantadine. Valganciclovir. similar to the development of pesticide resistance in insects. Consequently. The basic structure of fungal cells and human cells is nearly identical. or "noncovalent DNAbinding drugs". Anthracycline family: (Daunorubicin. Amphotericin B. The emergence of antivirals is the product of a greatly expanded knowledge of the genetic and molecular function of organisms. Bleomycin. Imidazoles and triazoles: inhibit the enzyme cytochrome P450 14ademethylase. 4. Imidazoles: Miconazole. Masoprocol. Trifluridine. Raltitrexed). Polyene antibiotics: bind with sterols in the fungal cell wall. Estramustine . Unlike bacteria. and the intense pressure placed on the medical profession to deal with the human immunodeficiency virus (HIV). Ravuconazole. This agent forms free radicals. Posaconazole. Peramivir. Fenticonazole. Doxorubicin. Ritonavir. Triazoles: Fluconazole. Cidofovir. Emtricitabine . if a small subset of the population survives the treatment and is allowed to multiply. Antifungals work by exploiting differences between mammalian and fungal cel ls to kill off the fungal organism without significantly harming the host. Bifonazole . Saquinavir. Zanamivir Abacavir. Tipranavir Enfuvirtide Adefovir. Nelfinavir. Tretinoin Antimetabolites: Plant alkaloids: Cytotoxic/antitu mor antibiotics: Topoisomerase inhibitors: Monoclonal antibodies: Photosensitizers: Other: 10 . This survival often results from an inheritable resistance to the compound which was infrequent in the original population but is now much more frequent in the descendants thus selected entirely from those originally infrequent resistant organisms. Oseltamivir. Ifosfamide. Butoconazole . plicamycin mitomycin Alkylating agents: Nitrogen mustards: ( Chlorambucil. which induce damage and chromosomal aberrations.3-ß glucan synthase: Anidulafungin. herpesvirus. Docosanol. In certain settings. Griseofulvin binds to polymerized microtubules and inhibits fungal mitosis.
and autoimmune disorders. reducing or eliminating their effectiveness. liver) treatment of autoimmune diseases or diseases that are most likely of autoimmune origin (e. mitramycin. that acts as a purine analogue and an inhibitor of DNA synthesis. platinum compounds and others. and be transported by the blood to a distant organ to exe rt its specific function. Polyclonal antibodies: Heterologous polyclonal antibodies are obtained from the serum of animals (e. and intracrine signals (a chemical that acts within the same cell). Clinically they are used to: prevent the rejection of transplanted organs and tissues (e. pyrimidine analogues and protein synthesis inhibitors. Antibodies: are used as a quick and potent immunosuppression method to prevent the acute rejection reaction. It is characterized by fever. T4) make up a subset of this class because they derive from the combination of two iodinated tyrosine amino acid residues. including graft rejection. they do not prevent an infection and also inhibit later reparative processes. joint pain and erythema that can be soothed with the use of steroids and analgesics. Mercaptopurine itself can also be administered directly. IL-4. ghrelin from the stomach. They are also administered as posttransplantory immunosuppressants to prevent the acute transplant rejection and graft-versus-host disease. Amines: such as norepinephrine. Thyroid hormones such as 3. Because of a high immunogenicity of polyclonal antibodies. potentiating the effect. Other cytotoxic antibiotics are anthracyclines.000. IL-8 and TNF-?. as are leptin from adipocytes . be released (in small amo unts) into the blood. rabbit . These include: folic acid analogues. Alkylating agents: are used in immunotherapy are nitrogen mustards (cyclophosphamide). Crohn's disease. horse) and injected with the patient's thymocytes or lymphocytes. respiratory burst and the release of various inflammatory mediators (lysosomal enzymes. dyslipidemia. Smaller cytokine production reduces the T cell proliferation. These drugs are not without side effects and risks. autoimmune hemolytic anemias. IL-6. They act by inhibiting genes that code for the cytokines IL-1. It binds dihydrofolate reductase and prevents synthesis of tetrahydrofolate. In immunotherapy. Steroids: are derivatived from cholesterol and are subdivided into those with an intact steroid nucleus (gonadal and adrenal steroids) and those with a broken steroid nucleus (vitamin D). mitomycin C. hyperglycemia. Serum sickness arises 7-14 days after the therapy has begun. All hormones secreted by the pituitary gland are peptide hormones.7. Monoclonal antibodies: are directed towards exactly defined antigens. 1. In this way. Three class es of hormone: 1. which is both complement mediated cytolysis and cell-mediated opsonization followed by removal of reticuloendothelial cells from the circulation in the spleen and liver]]. IL-5.0. 2. it affects both the cell and the humoral immunity. no matter what thei r cause.5. Endocrines and Immunosuppressants [2 Qs] The endocrine system consists of several glands. To be classified as a hormone. epinephrine. rheumatoid arthritis . In small doses. and insulin from the pancreas. Wegener's granulomatosis and other immune diseases.) from neutrophils .5.3’. Antimetabolites: interfere with the synthesis of nucleic acids. are derived from single amino acids. the most important of which is the IL-2. they are primarily added to other immunosuppressives to diminish their dosage and toxicity. emigration. It is possible to diminish their toxicity by using highly purified serum fractions and intravenous administration in the combination with other immunosuppressants. almost all patients have an acute reaction to the treatment. Cytostatics: inhibit cell division. Cyclophosphamide is probably the most potent immunosuppressive compound. causing B cells to express smaller amounts of IL-2 and of IL-2 receptors . the immune system loses its ability to successfully resist infections and spreading of malignant cells. The most frequent combination is to simultaneously use antibodies and cyclosporine. It is used in kidney transplantations.5’-tetraiodothyronine (thyroxine. Later during the treatment. mercaptopurine. bone marrow. These agents inhibit T lymphocytes and cause their lysis. IL-3. This leads to diminished eicosanoid production. inflammatory. The cyclooxygenase (both COX -1 and COX -2) expression is also suppressed. in this case tyrosine. They are part of the steroid-resistant acute rejection reaction and grave aplastic anemia treatment.3’triiodothyronine (T3) and 3. peptic ulcers . phagocytosis . and the graft-versus-host disease (GVHD). for example calcineurin inhibitors. (3) Cytotoxic antibiotics Among these. Peptides and Proteins: consist of three (in the case of thyrotropin-releasing hormone) to more than 200 (in the case of follicle-stimulating hormone ) amino acid residues and can have molecular weights as large as 30. cytostatics and cortisteroids. but there are also paracrine mechanisms (chemical communication between cells within a tissue or organ). where it binds to the leukocyte membrane receptors and inhibits various inflammatory events: epithelial adhesion . kidney. (1) Methotrexate: is a folic acid analogue. such as methotrexate purine analogues such as azathioprine and . bleomycin. High doses cause pancytopenia and hemorrhagic cystitis. Antiinflammatoryeffects Glucocorticoids influence all types of inflammatory events. dactinomycin is the most important. heart. These drugs suppress the cell-mediated immunity.e. It is nonenzymatically cleaved to mercaptopurine. but influence thymus-dependent antibody production. it is very efficient in the therapy of systemic lupus erythematosus. Immunosuppressive drugs or immunosuppressants are drugs that are used in immunosuppressive therapy to inhibit or prevent activity of the immune system. 11 . Immunosuppressive drugs can be classified into four groups and others: glucocorticoids cytostatics antibodies drugs acting on immunophilins other drugs Glucocorticoids: glucocorticoids are used to suppress various allergic. IL-2. The antilymphocyte (ALG) and antithymocyte antigens (ATG) are being used. myasthenia gravis. and dopamine. However. There are also other side effects. This definition holds for most ‘classical ’ hormones. 2. It is used in the treatment of autoimmune diseases (for exampl e rheumatoid arthritis) and in transplantations. some patients develop serum sickness or immune complex glomerulonephritis. cytokines. macrophages and mastocytes . Glucocorticoids also suppress the humoral immunity. The immunosuppressive drugs also interact with other medicines and affect their metabolism and action. nitrosoureas. which then binds to cell membranes preventing the phospholipase A2 from coming into contact with its substrate arachidonic acid. Nevertheless. delayed hypersensitivity (i. tissue plasminogen activator. like hypertension. Urticaria (hives) can also be present. testosterone from the testes. they cause fewer side effects. and ulcerative colitis). chemokines etc. autocrine signals (a chemical that acts on the same cell). The patient suffers from fever. Because the majority of them act non-selectively. (2) Azathioprine and Mercaptopurine: are is extensively used to control transplant rejection reactions. They also allow transition to cyclosporine therapy. Especially significant are the IL-2 receptor (CD25) and CD3 directed antibodies. tuberculin skin reaction). chemotaxis . It is reasonable to expect similar new drugs in the future. By preventing the clonal expansion of lymphocytes in the induction phase of the immune response. Patients gradually develop a strong immune response to these drugs.g.g. This diminishes both B cell clone expansion and antibody synthesis. and cortisol and aldosterone from the adrenal gland. liver and kidney injury. And include the alkylating agents and antimetabolites. They induce the lipocortin-1 (annexin-1) synthesis. Steroid horomones include estrogen and progesterone from the ovary. rigor episodes and even anaphylaxis. polyclonal antibodies inhibit cell-mediated immune reactions. They affect the proliferation of both T cells and B cells. a chemical must be produced by an organ. they are used in smaller doses than in the treatment of malignant diseases. 3. that secrete hormones directly into the blood rather than into a duct system. 1. Glucocorticoids also stimulate the lipocortin-1 escaping to the extracellular space. Therefore.g. but also to track changes in the lymphocyte subpopulations. They are used to prevent the rejection of transplant ed organs. 2. systemic lupus erythematosus.
Indometacin. selective and reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH). with this action associated with spinal analgesia and miosis. it is one of the most potent immunosuppressive substances and is clinically used to control the steroid and/or polyclonal antibodies resistant acute rejection episodes. It also decreases hunger. preventing the IL-2 induced clonal expansion of activated lymphocytes and shortening their survival. as it is nephrotoxic. The IL-2a (CD25. headache and artralgia. Crohn's disease and psoriasis. has few side effects. euphoria. especially T-lymphocytes. Cyclosporin is used in the treatment of acute rejection reactions. As such. consisting of the a. Piroxicam Celecoxib . Presently. Opioids 8. These drugs may raise the risk of contracting tuberculosis or inducing a latent infection to become active. It is characterized by fever. CD3 antibodies also shift the balance from Th1 to Th2 cells. Etoricoxib . TNF or the effects of TNF are also suppressed by various natural compounds. In this way. It increases the expression or changes the function of certain adhesion molecules ( a4/ß7 integrin) in lymphocytes. including curcumin (an ingredient in turmeric) and catechins (in green tea). Activation of these receptors is associated with analgesia. IL-2 receptor directed antibodies: is an important immune system regulator necessary for the clone expansion and survival of activated lymphocytes T. Opioids: Prolonged use of opioids may cause immunosuppression by inhibiting the migration of leukocytes. Tacrolimus is more potent than cyclosporin and has less pronounced side effects. Sulindac Carprofen . They are used in the treatment of rheumatoid arthritis. ly mphocytes B and T are very dependent on this process. it dif fers from all other known immunosuppressants. It is a fungal peptide. followed by the binding of the complex to calcineurin and the inhibition of its phosphatase activity. 8. Therefore.1. Infliximab and adalimumab have label warnings stating that patients should be evaluated for latent TB infection and treatment should be initiated prior to starting therapy with them. It is used to prevent rejection reactions. it prevents the passage of G0 into G1 phase. Flurbiprofen . Mefenamic acid Phenylbutazone Meloxicam. sirolimus affects the second one. ankylosing spondylitis. etanercept (Enbrel ®). This lowers the number of T cells. Loxoprofen . lung and heart/lung transplants. so they accumulate in the lymphatic tissue (lymphatic nodes) and their number in the circulation is diminished. Tacrolimus (Prograf(TM): is a bacterial product (Streptomyces tsukubaensis). produced by the actinomycetes Streptomyces hygroscopicus. Similarly.6 and the adhesion of lymphocyte activating molecules. this binding non-specifically activates T cells. Drugs acting on immunophilins Cyclosporin: Together with tacrolimus.2. Arylalkanoic acids 2-Arylpropionic acids (profens) N-Arylanthranilic acids (fenamic acids) Pyrazolidine derivatives Oxicams Coxibs Sulphonanilides Diclofenac. It is a mouse anti-CD3 monoclonal antibody of the IgG2a type that prevents T-cell activation and proliferation by binding the T-cell receptor complex present on all differentiated T cells. Analgesics [5 Qs] 8. preventing the transmission of signal into their activity and the transition of the cell cycle from G1 to S phase. It binds to an immunophilin. heroin. and blurred vision. Past this period.3. Valdecoxib Nimesulide 12 . It binds to the same receptor (immunophilin) as tacrolimus. Naproxen . T-cell activation antigen. namely the signal transduction and their clonal proliferation. By the use of the recombinant gene technology. perhaps by sensitising them for the uptake by the reticular epithelial cells. Parecoxib. For acting more specifically than polyclonal antibodies. unless they receive another signal through a costimulatory molecule. CD3 (R) blocks the TCR . TNF binding proteins: A TNF -a (tumor necrosis factor alpha) binding protein is a monoclonal antibody or a circulating receptor such as infliximab (Remicade®). Morphine is highly addictive when compared to other substances. Ketoprofen . physical dependence and respiratory depression. They are used in the profilaxis of the acute organ rejection after the bilateral kidney transplantation. Morphine is also a ?-opioid receptor agonist. Tiaprofenic acid. Its eff ects are mediated by the trimer cell surface receptor IL-2a. sedation. Morphine is primarily metabolized into morphine-3-glucuronide and morphine-6-glucuronide. In contrast to other human cell types. drowsiness. The effects of morphine can be countered with naloxone or naltrexone. It acts immunoregulatory. These drugs act by binding the IL-2a receptor's a chain. Mycophenolate: Mycophenolic acid acts as a non-competitive. Side effects include impairment of mental performance. Morphine is an opioid receptor agonist – its main effect is binding to and activating the µ-opioid receptors in the central nervous system. the mouse anti-Tac antibodies have been modified leading to the presentation of two himeric mouse/human anti-Tac antibodies in the year 1998: basiliximab (Simulect (R)) and daclizumab (Zenapax (R)). Rofecoxib. It has been in use since 1983 and is one of the most widely used immunosuppressive drugs. it progresses to a life-threatening reaction of the cardiovascular system and the central nervous system needing a lengthy therapy. morphine acts directly on the central nervous system (CNS) to relieve pain. The drug also inhibits lymphokine production and interleukin release. IgG and IgA antibodies produced. Cyclosporin is thought to bind to the cytosolic protein cyclophilin (an immunophilin) of immunocompetent lymphocytes. which lowers the quantity of IgM. This complex of ciclosporin and cyclophilin inhibits calcineurin. but another protein.antigen binding and causes conformation change or the removal of the entire TCR3/CD3 from the T-cell surface. euphoria. Ketorolac. It is known that the molecule binds TCR/CD3. however the produced complex does not inhibit calcineurin. Although it is a structural analogue of tacrolimus. It is used to slow down the progression of multiple sclerosis. the OKT3's action mechanism is not yet sufficiently understood. it acts somewhat differently and has different side effects. TAC) is expressed only by the already activated T lymphocytes. it is of special significance to the selective immunosuppressive treatment and the research has been focused on the development of effective and safe anti-IL-2 antibodies. the Tcell receptor complex. Indirectly it inhibits several T lympohocyte kinases and phosphatases.  Small biological agents FTY720 is a new synthetic immunosuppressant. Therefore.g. leading to a reduced function of effector T-cells.0. causing the T cells' anergy or apoptosis. Contrary to cyclosporine and tacrolimus that affect the first phase of the T lymphocyte activation. inhibits the cough reflex. Sirolimus (Rapamune(Tm). lethargy. and produces constipation. or adalimumab (Humira®) that binds to TNF . but has been increasingly substituted with newer immunosuppressants. which is a key enzyme in the de novo guanosine nucleotide synthesis.1 and IL. although in some clinics it is used in heart. In this respect. composed of 11 amino acids. it is also used preventively in transplantations. Other drugs Interferons IFN-ß suppresses the production of Th1 cytokines and the activation o : f monocytes. which under normal circumstances induces the transcription of interleukin-2. ß and ? chains. During the first few administrations. Rapamicin): Sirolimus is a macrolide lactone. T-cell receptor directed antibodies OKT3 (R) is presently the only approved anti-CD3 antibody. leading to a serious syndrome 30 to 60 minutes later. myalgia. NSAIDs Non-steroidal anti-inflammatory drugs Morphine is an extremely powerful opiate analgesic drug and is the principal active agent in opium. cyclosporin is a calcineurin inhibitor. In some cases. e. It is a macrolide lactone and acts by inhibiting calcineurin. and tolerance and physical and psychological dependence develop quickly. IFN-? is able to trigger lymphocytic apoptosis.a and prevent it from inducing the synthesis of IL. sirolimus acts synergistically with cyclosporine and. Non-opioids. it prevents the B cell differentiation to the plasma cells. The cross-binding of CD3 molecules also activates an intracellular signal. Like other opioids. High doses of morphine may be fatal due to respiratory depression. The drug is used particularly in the liver and kidney transplantations. in combination with other immunosuppressants. Ibuprofen . currently in phase 3 of clinical trials.
Antihistamines (H1 receptor antagonists): Widely used for hay fever. Suppresses the itching and pain Other effects: CNS depression (Sominex. Anticholinergic . Diamorphine (Heroin). and Ethenzamide derivatives: Pyrazolones: Anilides: Others: Aminophenazone. Codeine. elderly with larger doses. Nytol). Metamizole. Butorphanol . bronchoconstriction. OTC sleep aids. Ketobemidone. this will decrease BP severely causing shock and CV collapse. lapses into unconsciousness. Bonine). Tetrahydrocannabinol Autocoids and Antihistamines Autocoid agonists or antagonists include: -H1 and H2 receptor antagonists -Eicosanoids (prostaglandins) -Thromboxanes -Leukotensin -Serotonin agonists -Angiotensin inhibitors -Cytokinins -Histamine NOTE: Histamine is released during allergic reactions. Tramadol 9. Uses: Control seasonal hay fever. of certain drugs and amount released determines effects. Adverse effects includes: Anaphylaxis – serious and sometimes fatal. if high levels of histamine released. Fentanyl . The End & Good Luck 13 . Drug of choice to counteract histamine rxn is epinephrine. Oxymorphone. Pentazocine. Hydromorphone. Pethidine (Meperidine). Antihistamines and Autocoids [2 Qs] Salicylic acid Aspirin (Acetylsalicylic Acid). mild allergic reactions and additive with other CNS depressants Four common: Dipheniramine (Benedryl ).0. Loratidine (Claritin) Pharmacologic effects: H1 blocking effects include: Capillary permeability is blocked producing reduced edema. More common in children. Sedative effect cancelled out when combined with decongestant (adrenergic agonist). To prevent and treat motion sickness Preop sedation and antiemetic effects. or after admin. Dihydrocodeine. Phenacetin Ziconotide. H2-agonist effect includes increased gastric acid secretion. pain or itching. vasodilation and increased capillary permeability. Uses include: diagnosis of achlorhydria and pheochromocytoma. Diflunisal. edema and erythema Some topical anesthetic effect. CNS stimul ation can occur in a few cases. Xerostomia Toxicity: More common due to easy accessibility in OTC preparations Death can result. Relieve itching. Phenazone Paracetamol (acetaminophen). Antiemetic (Dramamine. Morphine. Hydrocodone.Analgesics Opioids : Buprenorphine. Nalbuphine. immune reactions. Promethazine (Phenegan). difficulty breathing. Chlorphenhydramine (ClorTrimeton). Dextropropoxyphene. Oxycodone. increased capillary permeability. Pharmacologic effects: H1-agonists produce vasodilation. convulsions. Newer nonsedating H1 blockers (Clariton) produce less sedation. Blocks dilation of vascular smooth muscle. Adverse reactions: Undesirable CNS depression. Blocks some bronchoconstriction.
Show a plot of drug concentration versus time that is linear Question: Why or When do we use drugs (clinically)? Answer: To control. or prevent disease Question: Who can prescribe drugs. Cytochrome P450 reaction B. Question: What can you Rx? Answer: Drugs within the scope of your practice Answer: Drugs within the scope of your practice 14 . Are more common than those showing first-order kinetics B. and Where? Answer: Licensed doctors. Transformation reaction C. Have a half-life that is independent of dose D.The conjugation of glucuronic acid to a drug by the liver is an example of a: A. Phase I activation reaction D. cure. Phase II inactivation reaction Drugs showing zero-order kinetics of elimination: A. Decrease in concentration exponentially in time C. requires DEA registration and is state specific.
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