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Routes that do not make use of the alimentary canal. 1. Injection 2. Pulmonary 3. Topical |
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Routes that use the alimentary canal (oral and rectal) |
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INJECTION Putting drug directly in the bloodstream PROS Accuracy of dosage and speed of delivery CON Cannot retrieve drug in case of overdose or allergic reaction. Also must worry about sterilization |
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INJECTION Under the skin by injection or implants (in solid form) |
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INJECTION Injection of drug into a ________ mass, usually arm or butt. Slower absorption |
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INJECTION For pain management, drugs are injected directly onto the spinal cord. Keeps drug confined to very small area. Two types: epidural (just outside the protective layers surrounding the spinal cord); spinal anesthetics (directly onto the spinal cord) |
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SWALLOWING (Enteral) 1. if person is unwilling or unconscious 2. if person is vomiting 3. contents of stomach determine level of absorption 4. stomach acid may interfere |
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Enteral Has enormous variability of absorption. |
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Use of a hypodermic syringe
1. IV 2. IM 3. SQ 4. Central Nervous System |
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Inhaling a drug (another parenteral route) NOT SNORTING Absorption is rapid Shortest route to brain |
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Laying a drug onto a body surface, usually a mucous membrane
1. Sublingual 2. Intranasal 3. On the skin (DMSO) |
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TOPICAL Placing a drug under the tongue. If some is swallowed, then it is enteral. |
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TOPICAL Intense inhalation of a drug, usually in powdered form, through the nostril. Does not reach the lungs but lays on the olfactory mucousal membranes of the nose. |
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TOPICAL DMSO (dimethyl sulfoxide) is an efficient solvent and if drugs are dissolved in it, the drug can be absorbed through skin contact |
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Neurotransmitter receptors Enzymes Membrane Transport Mechanisms |
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Membrane Transport Mechanisms |
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Some cells have ___________ in their membranes that have the function of transporting items across the cell membrane. Certain drugs bind to the proteins and prevent cellular movement. |
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Receptors for Neurotransmitters |
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Target surface has specialized proteins that bind _______ and drug molecules can bind to these receptors and change the interactions that normally result. |
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Some _____ can bind drug molecules and have their energy changed as a result. Sometimes the normal activity is blocked. |
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SOMETIMES means most intense effect. Usually means the effect that is of most interest to the author.
"One persons main effect is another's side effect" |
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The effective dose (shows the desired behavior) is __ (#) % of the population. |
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LD-50/ED-50 The larger the number, the less likely you are to die, the safer the drug dosage.
Measures how close you are to the LD (small number = close) |
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1. Enters the body 2. Distributes through the body 3. Excreted in a changed or unchanged form 4. All the while, interacting with receptors |
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Any exogenous substance or compound |
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What do all of the body compartments have in common? |
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They must make contact with the blood. The blood reaches every compartment in the body. |
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The time from the administration of a drug to the time is reaches the blood circulation. |
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What protein do drugs bind to in the blood? |
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Hydrophobic Fat The cell membrane is a double layer of lipids |
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Hydrophilic Part of membranes |
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Basic dilemma for the brain? |
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Needs more nutrients from the blood than any other organ YET must be the most protected from the toxins in the blood--hence the Blood-Brain Barrier |
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Fast, but not as fast as IV Inhalation has the shortest route to the brain, however |
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1. Capillaries are specialized so they have virtually no gaps between them 2. Glial cells protect the neurons so the drugs must go through the glial cells before they reach the neuron.
AS A RESULT.. drugs must be highly lipid-soluble |
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1. Lungs 2. Liver (accumulate in bile) 3. Fluid (sweat, mom's milk) |
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Those products produced in the process of biotransforming a drug which are psychoactive themselves
Drug A --> biotransformation --> Drug A' (still activates receptors and has effects) |
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The time it takes for half the initial dose of a drug to be cleared from the blood |
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Approximation of Clearance |
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4 1/2 half-lives
96% of the drug is cleared. If you dose more often that 4 1/2 half-lives, then you will accumulate drugs in your system |
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1. Must bind drug molecule 2. Presence of the bound drug molecule must alter some normally occurring physiological event
--> if not change, NOT a receptor |
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