Biochemical Pharmacology

Introduction

What is `biochemical pharmacology'?
What are drugs?
Drugs and drug target molecules
Drug molecules may or may not have physiological counterparts
Synthetic drugs may exceed the corresponding physiological agonists in selectivity
Metabolism of physiological mediators and of drugs
Strategies of drug development

Pharmacokinetics

Pharmacokinetics
Drug application and uptake - Pharmacokinetics
Drug distribution - Pharmacokinetics
Drug elimination: Kidneys
Drug elimination: Metabolism

Pharmacodynamics

Pharmacodynamics
Classes of drug receptors
Mechanisms and kinetics of drug receptor interaction
Drug dose-effect relationships in biochemical cascades
Spare receptors
Potency and efficacy
Partial agonism and the two-state model of receptor activation
Toxic and beneficial drug effects

The ionic basis of cell excitation

The ionic basis of cell excitation
Ion gradients across the cell plasma membrane
The physics of membrane potentials
Voltage-gated cation channels and the action potential
The origin of cell excitation
Anion channels

Drugs that act on sodium and potassium channels

Drugs that act on sodium and potassium channels
Local anesthetics
Sodium channel blockers as antiarrhythmic agents
Sodium channel blockers in epilepsia
Potassium channel blockers
Potassium channel openers

Some aspects of calcium pharmacology

Some aspects of calcium pharmacology
Calcium in muscle cell function
Calcium channel blockers
Digitalis (foxglove) glycosides
Calcium-dependent signaling by adrenergic receptors

Some aspects of neurophysiology relevant to pharmacology

Some aspects of neurophysiology relevant to pharmacology
Structure and function of synapses
Mechanisms of drug action on synapses
Pharmacologically important neurotransmitters and their receptors
Neurotransmitter receptors
Overview of the autonomic nervous system

G protein coupled receptors

G protein-coupled receptors
Structure and function of G protein-coupled receptors
The complexity of G protein signalling
Agonist-specific coupling
GPCR oligomerization
'Allosteric' GPCR agonists and antagonists

Pharmacology of cholinergic synapses

Pharmacology of cholinergic synapses
Structure and function of the nicotinic acetylcholine receptor
Cholinergic agonists
Cholinergic antagonists
Cholinesterase antagonists

Pharmacology of catecholamines and of serotonin

Pharmacology of catecholamines and of serotonin
Biosynthesis and degradation of catecholamines
Pharmacokinetic aspects
Drug targets in catecholaminergic synapses
Adrenergic receptor agonists and antagonists
Inhibitors of presynaptic transmitter reuptake
Inhibition of vesicular storage
Indirect sympathomimetics
L-DOPA and carbidopa in the therapy of Parkinson's disease
False transmitters
Cytotoxic catecholamine analogs
Monoamine oxidase inhibitors

Pharmacology of nitric oxide NO

Pharmacology of nitric oxide (NO)
Vascular effects of nitric oxide
Nitric oxide synthase and its isoforms
Biochemical mechanisms of NO signaling
Role of NO in macrophages
NO releasing drugs
NOS inhibitors

Pharmacology of Eicosanoids

Pharmacology of Eicosanoids
Biosynthesis of eicosanoids
Cyclooxygenase inhibitors
Lipoxygenases and related drugs

Some principles of cancer pharmacotherapy

Some principles of cancer pharmacotherapy
Cell type-specific antitumor drugs
The cell cycle
Alkylating agents
Antibiotics
Antimetabolites
Inhibitors of mitosis
Monoclonal antibodies in tumour therapy

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