UNIVERSITY OF SPLIT

SCHOOL OF MEDICINE

PHARMACOLOGY

LITERATURE:

Katzung BG, Masters S, Trevor AJ. Basic and Clinical Pharmacology 12th edition. New York: McGraw-Hill Medical; 2012

EXAM MATERIAL FROM THE TEXTBOOK

The purpose of this student material is assistance for better understanding of an otherwise comprehensive textbook while preparing for the exam in pharmacology. Entire chapters or sections of chapters that will not be in the exam are marked, and parts needing special attention are highlighted. The referred generic names are typical representatives of a particular drug group and they represent the majority of the drugs to be memorized for the final exam. The summary table at the end of each chapter should be used for information about different drug groups.

Chapter 1

Completely. It is not necessary to remember data in the tables.

Chapter 2

Completely. It is not necessary to remember table data.

Chapter 3

Completely. It is not necessary to remember numeric data in the tables

Framed text “Maintenance dose calculations” and “The target concentration strategy” can be test material.

Chapter 4

Completely. It is not necessary to remember examples from table 4-1, 4-3, 4-4 and 4-7. Note in table 4-2 CYP3A4, 1A2, 2C9, 2C19, 2D6, the enzymes metabolizing the majority of drugs in context of main interactions and genetic factors that influe their enzymatic activity.

Chapter 5

Completely. Table 5-2 is not test material

Chapter 6

Completely.

Chapter 7

Completely.

-  Direct-acting cholinoreceptor stimulants: mechanism of action, organ system effects, basic pharmacokinetics and main representatives (pilocarpine i bethanechol).

-  Indirect-acting cholinomimetics: mechanism of action, organ system effects, basic pharmacokinetics and main representatives (neostigmine, edrophonium, physostigmine, organophosphates).

Clinical pharmacology of cholinomimetics: main indication and basic information about adverse effects.

Chapter 8

Subtitle „Basic and clinical pharmacology of the ganglion-blocking drugs” is not test material. Concentrations in table 8-2 and usual dosage from table 8-3 do not to be memorized.

Basic pharmacology of the muscarinic receptor-blocking drugs: mechanism of action, organ system effects, basic pharmacokinetic, main representatives, main indications for administration and adverse drug reactions (ADRs).

-  Pay special attention to: atropine, ipratropium, tiotropium, tropicamide, scopolamine, butylscopolamine i trospium.

Chapter 9

Completely.

In table 9-1 it is not necessary to memorize the chromosome of the receptor and from table 9.5 the quantity of tiramine.

Therapeutic use of sympathomimetic drugs: focus on indications (shortly!) and rational basis for administration. The text in the frame „An application of basic pharmacology to a clinical problem” can be exam material.

-  Special attention: phenylephrine, ritodrine; salbutamol i salmeterol (see also in chapter 20), fenoldopam, methyldopa, clonidine (see also in chapter 11.)

-  Sympathomimetics with mixed effects: ephedrine.

Basic adverse drug reactions (ADRs).

Chapter 10

Completely.

In subtitles „Clinical pharmacology of the alpha-receptor blocking drugs” and „ Clinical pharmacology of the beta-receptor blocking drugs” focus on the indications (shortly), rational basis for administration and basic adverse drug reactions (ADRs), (toxicity)

The text in the frame „The treatment of glaucoma” can be exam material.

-  Special attention to adreno-receptor antagonists: phenolamine, doxazosin, tamsulosin; atenolol, metoprolol, propranolol, bisoprolol, carvedilol, timolol, nebivolol, sotalol.

Chapter 11

Subtitle „Clinical pharmacology of antihypertensive agents” is not exam material. In table 11-2 drug dosage is not necessary.

-  Drugs influencing sodium, potassium and water balance (see also chapter 15)

-  Drugs modifying sympathic nerve system function: sympathoplegic drugs with central activity (particularly methyldopa, clonidine); adrenoceptor antagonists (see chapter 10.)

-  Vasodilators: hydralazine, minoxidil, sodium nitroprusside, diazoxide, fenoldopam (basic pharmacodynamic characteristics and indications)

-  Calcium channel blockers: basic pharmacodynamics, pharmacokinetics, main therapeutic indications and ADRs, particularily: verapamil, diltiazem, nifedipine, amlodipine, lacidipine, nimodipine (see chapters 12 and 14)

-  Angiotensin-converting enzyme (ACE) inhibitors:

-ACE inhibitors: haemodynamic and other effects of this drug group, main clinical indications and ADRs (particularily enalapril, lisinopril, ramipril); (also see chapter 13)

-Angiotensin receptor-blocking agents: haemodynamic and other effects of angiotensin receptor blockage, clinical indications and ADRs, (i.e. losartan and valsartan); (also see chapter 13.)

-Renine inhibitors: aliskiren (see p.297-298 in chapter 17)

-Aldosterone antagonists (see also chapter 15: potassium-sparing diuretics- spironolactone, eplerenon)

Chapter 12

Subtitle „Newer antianginal drugs” and data in table 12-6 are not exam material. It is not necessary to memorize drug dosage in tables 12-5 and 12-3. Frame text „Drugs used in the treatment of erectile dysfunction” can be exam material.

- Pay special attention to:

- nitrates and nitrites (nitroglycerin, isosorbide mononitrate, isosorbide dinitrate), mechanism of action, organ system effects, main indications for administration and adverse drug reactions (ADRs).

(see also chapter 13.)

- drugs used in the treatment of erectile dysfunction (sildenafil, p199), interactions with nitrites

- calcium channel blockers (like in chapter 11)

- beta blockers: see also chapters 10 and 11

Clinical pharmacology of drugs used to treat angina: explanation of table 12-7

Chapter 13

Subtitle „Pathophysiology of cardiac performance” is not exam material, but is advisable to read for better understanding of heart failure treatment pharmacology.

In the subtitle „Clinical pharmacology for the treatment of heart faulire” focus on specific drugs/groups used in acute and chronic heart failure, not on the principals of pharmacotherapy. Table 13-3 should be studied only on an informative level.

Basic pharmacology of drugs for heart failure:

- digitalis (digoxin), mechanism of action, cardial and extracardial effects, indications and ADRs.

- other positive inotropic drugs used in heart faulire: i.e. milrinone, levosimendan, dobutamine, dopamine, (see also chapter 9)

Drugs without positive inotropic effects used in heart failure:

- especially loop diuretics and aldosterone antagonists (see also chapter 15)

- ACE inhibitors and ARBs angiotensin receptor blockers (see also chapters 11 and 12)

- nesiritide; bosentan

Chapter 14

Subtitle “Basic pharmacology of the antiarrhythmic agents” is not exam material. Further subtitles “Electrophysiology of normal cardiac rhythm” and „Mechanisms of arrhythmias” are also not exam material, but are recommended for better understanding of antiarrhythmic agents pharmacology.

Data in table 14-1 is not test material. Texts in frames “The nonpharmacologic therapy of cardiac arrhythmias” and „Antiarrhythmic drug-use principles applied to atrial fibrilation” are not test material.

Pay special attention to the following antiarrhythmic drugs:

- sodium channel-blocking drugs (class 1): disopyramide (1A), lidocaine (1B), propafenone (1C)

- beta adrenoreceptor-blocking drugs (class 2): propranolol, sotalol (see also chapter 10, 11 and 12)

- drugs that prolong effective refractory period by prolonging the action potential (class 3): amiodarone (sotalol)

- calcium channel-blocking drugs (class 4): verapamil

- miscellaneous antiarhythmic agents: digoxine (see also chapter 13.), adenosine, potassium, magnesium

Chapter 15

Completely. Not necessary to memorize data from tables 15-3, 15-4, 15-5 and 15-6.

Subtitle “Basic pharmacology of diuretic agents”, focus on main indications.

- carbonic anhydrase inhibitors, mechanism of action, indications and ADRs (acetazolamide, dorzolamide).

- loop diuretics, mecanism of action, indications and ADRs (furosemid, torasemid).

- thiazides, mecanism of action, indications and ADRs (see chaper 11), hydrochlorothiazide, chlortalidone, indapamide.

- potassium sparing diuretics, mecanism of action, indications and ADRs, amiloride, triamterene, spironolactone, eplerenone.

- osmotic diuretics, mannitol, indications and contraindications.

Chapter 16

Subtitles “Basic pharmacology of histamine and basic pharmacology of serotonine” are not test material but advised to read for better undersanding of the drugs described in the chapter. In tables 16-2 and 16-5 dosages do not need to be memorized.

Subchapter “Histamine receptor antagonists” completely.

In the subtitle “Clinical pharmacology” focus on indications (shortly) ADRs and toxicity:

-  particularily: diphenhydramine, dimenhydrinate, loratadine, fexofenadine

-  from chapter „Serotonine”, test material is subtitle “Clinical pharmacology” in the part called “Serotonine agonists”. Focus on the text “5-HT1B/D agonists and migrene” (particularly sumatriptan and zolmitriptan).

-  further: buspirone (see chapter 22) ;

-  antagonists: ondansetron (see also in chapter 62).

-  subchapter „Ergot alkaloids” completely. In subtitle „Clinical pharmacology of ergot alkaloids” focus on main indications (shortly) and ADRs (toxicity). Pay special attention to: ergometrine (ergonovine), bromocriptine

Chapter 17

Only subchapter “Angiotensin”

Chapter 18

Not exam material. However, this chaper is a useful reminder on the physiology and biochemistry of eicosanoids which may be helpful for better understanding of NSAID and drugs used in the treatment of asthma.

Chapter 19

Is not test material; useful reminder of nitric oxide physiology.

Chapter 20

Subtitle “Clinical pharmacology of drugs used in the treatment of asthma” is not exam material.

Use summary table at the end of the chapter for better distuingshment of drug groups used. Pay special attention to:

-  sympathomimetics: adrenaline (epinephrine), salbutamol, salmeterol

-  methylxanthines: theophylline, aminophylline

-  antimuscarinic agnets: ipratropium bromide, tiotropium bromide

-  corticosteroids (inhalation): fluticasone, mometasone, budesonide

-  stabilizers of cells: cromolyn, nedocromil

-  leukotriene inhibitors: montelukast, zafirlukast

-  IgE antibody: omalizumab

Chapter 21

Is not test material.

Chapter 22

Completely. In subtitle “Clinical pharmacology of sedative-hypnotics” focus on main indications shortly and ADRs (toxicity).

Pay special attention to:

- benzodiazepines: i.e. diazepam, alprazolam, triazolam, oxazepam, midazolam (see chapter 25), clonazepam (see chapter 24); antagonist flumazenil

- barbiturates: phenobarbital (see chapter 24.), thiopental (see chapter 25.).

- newer hypnotics: zolpidem

- miscellaneous: buspirone (see chapter 16).

- ramelteon

Chapter 23

Is not test material.

Chapter 24

Basic pharmacology of antiseizure drugs: molecular targets for antiepileptics, figure 24-1 and 24-2, mechanism of action and ADRs.

-  From drugs used in partial and generalized tonic-clonic seizures focus on phenytoin

(mechanism of action, pharmacokinetics, ADRs, interactions with other drugs, clinical uses, carbamazepine, phenobarbital (see also in chapter 22), lamotrigine, vigabatrin, levetiracetam.

-  From drugs used in generalized seizures focus on ethosuximide (mechanism of action, pharmacokinetics, ADRs, interactions with other drugs, clinical uses), valproic acid /sodium valproate

-  Other drugs used in management of epilepsy, focus on benzodiazepines, clonazepam and diazepam, i.e. (detailes about of action, pharmacokinetics, ADRs, interactions with other drugs, see chapter 22).

In subchapter “Clinical pharmacology of Antiseizure drugs”, subtitle “Seizure classification” and “Management of epilepsy” are not test material.

Subtitle “Special aspects of the toxicology of Antiseizure drugs” is test material.

Chapter 25

Completely. The frame text ”Sedation & monitored anestesia care” is not test material.

-  Inhaled anesthetics: nitrous oxide, halothane,sevoflurane, pharmacokinetics and ADRs

-  Intravenous anesthetics: barbiturates; thiopental (see chapters 22 and 24), benzodiazepines; midazolam (see chapter 22), propofol; fentanyl, ketamine: mechanism of action, indications, ADRs

-  Tables 25-1 and 25-2 are not exam material.

Chapter 26

Completely. In subchapter “Clinical pharmacology of local anesthetics” focus on the paragraph “Toxicity”. Data in tables 26-1 and 26-2 do not have to be memorized.

Basic pharmacology of local anesthetics: lidocaine (see chapter 14), bupivacaine, procaine.

Chapter 27

Basic pharmacology of neuromuscular blocking drugs: mechanism of action, indications, ADRs, antidots:

- nondepolarizing relaxant drugs: pancuronium, tubocurarine

- depolarizing relaxant drugs: succinylcholine

- spasmolitics: diazepam (also see chapter 22), dantrolene, botulinum toxin (see chapter 6)

Chapter 28

Introduction and subtitle “Parkinsonism” are not test material, but are recmomendded for better understaning of the drugs described in this chapter. Focus on the pharmacology of the drugs used for Parkinsonism.

Likewise, drugs in the subtitle “Other movement disorders” are not test material. The text in the frame “MPTP Parkinsonism” is not test material.

Pay special attention to basic mechanism of action of:

- levodopa + carbidopa (mechanism of action, ADRs)

- dopamine receptor agonists: bromocriptine, pramipexole

- MAO inhibitors: selegiline

- COMT inhibitors: entacapone

- amantadine

- anticholinergic drugs: biperiden, benztropine

Chapter 29

Subtitle “Nature of psychosis & schizophrenia” and the hypothesis of schizophrenia are not test material but recommended for better understanding of antipsychotic agents and their mechanism of action.

In the subtitle “Clinical pharmacology of antipsychotic agents” focus only on indications and ADRs. Choice, dosage, regimes and maintenance treatment are not test material including table 29-4.

In the paragraph “Lithium, mood-stabilizing drugs & other treatment for bipolar disorder” focus on the text in “Basic pharmacology of lithium”. In the text “Clinical pharmacology of lithium” focus on indications, interactions and ADRs.

Pay special attention to:

- classic antipsychotics: chlorpromazine, thiothixene, haloperidol

- atypical - newer: clozapine, risperidone, olanzapine

- valproic acid and carbamazepine (also see chapter 24)

Chapter 30

Hypothesis of the depression pathophysiology are not test material but advised for better understanding of antidepressants mechanism of action.

Completely „Basic pharmacology of antidepressants”

Pay special attention to

- selective serotonin reuptake inhibitors: fluoxetine and sertraline

- serotonin-norepinephrine reuptake inhibitors:

- selective: venlafaxine

- tricyclic: imipramine, amitriptyline

- 5-HT2 antagonists: trazodone

- tetracyclic and monocyclic: mirtazapine, bupropion

- MAOIs: selegiline (see also chapter 28), moclobemide

In the subtitle “Clinical pharmacology of antidepressants” focus on indications, ADRs, overdose and interactions. “Choosing an antidepressant and dosage” are not test material including data in table30-1 to 30-3. Table 30-4 is only informative.

Chapter 31

Pharmacodynamics: mechanism of action of opioids figures 31-1 to 31-4.

Clinical use of Opioid analgesics, ADRs

Text in the frame “Ion channels & novel analgesic targets” is not test material.

Specific drugs:

- strong agonists: morphine, heroine, methadone, fentanyl (see also chapter 25)

- partial agonists: codeine, oxicodon, loperamide (see also chapter 62)

- mixed agonists/antagonists: buprenorphine, pentazocine

- other: tramadol

- antitussives: codein, dextromethorphan

- antagonists: naloxone

Chapter 32

Basic pharmacology of drugs of abuse:

- opioidis (see also chapter 31)

- cannabinoids

- LSD

- gamma-hydroxybutyric acid

- barbiturates – alcohol, benzodiazepines

- cocaine

- amphetamines

- ecstasy

Subtitle “Basic neurobiology of drug abuse” is not test material but recommended for better understanding. Same goes for text in frames “The dopamine hypothesis of addiction” and “Sinaptic plasticity & addiction”.

Chapter 33

Agents used in anemias:

- iron: oral and parenteral preparations, pharmacokinetics and ADRs